Vitekta

1 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

ANNEX I 
 

SUMMARY OF PRODUCT CHARACTERISTICS 

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This medicinal product is subject to additional monitoring.  This will allow quick identification of 
new safety information.  Healthcare professionals are asked to report any suspected adverse reactions.  
See section 4.8 for how to report adverse reactions. 
 
1. NAME OF THE MEDICINAL PRODUCT 
 
Vitekta 85 mg film-coated tablets 
 
 
2. QUALITATIVE AND QUANTITATIVE COMPOSITION 
 
Each film-coated tablet contains 85 mg of elvitegravir. 
 
Excipient with known effect: Each tablet contains 6.2 mg lactose (as monohydrate). 
 
For the full list of excipients, see section 6.1. 
 
 
3. PHARMACEUTICAL FORM 
 
Film-coated tablet (tablet). 
 
Green, pentagon-shaped, film-coated tablet of dimensions 8.9 mm x 8.7 mm, debossed with “GSI” on 
one side of the tablet and “85” on the other side of the tablet. 
 
 
4. CLINICAL PARTICULARS 
 
4.1 Therapeutic indications 
 
Vitekta co-administered with a ritonavir-boosted protease inhibitor and with other antiretroviral 
agents, is indicated for the treatment of human immunodeficiency virus-1 (HIV-1) infection in adults 
who are infected with HIV-1 without known mutations associated with resistance to elvitegravir (see 
sections 4.2 and 5.1). 
 
4.2 Posology and method of administration 
 
Therapy should be initiated by a physician experienced in the management of HIV infection. 
 
Posology 
Vitekta must be administered in combination with a ritonavir-boosted protease inhibitor. 
 
The Summary of Product Characteristics for the co-administered ritonavir-boosted protease inhibitor 
should be consulted. 
 
The recommended dose of Vitekta is one 85 mg tablet or one 150 mg tablet taken orally once daily 
with food.  The choice of dose of Vitekta depends on the co-administered protease inhibitor (see 
Table 1 and sections 4.4 and 4.5).  For use of the 150 mg tablet, please refer to the Summary of 
Product Characteristics for Vitekta 150 mg tablets. 
 
Vitekta should be administered once daily as follows: 
- Either at the same time as a once daily ritonavir-boosted protease inhibitor 
- Or with the first dose of a twice daily ritonavir-boosted protease inhibitor. 
 

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Table 1: Recommended dosing regimens 
 
Dose of Vitekta Dose of co-administered ritonavir-boosted protease inhibitor 

85 mg once daily 
atazanavir 300 mg and ritonavir 100 mg once daily 

lopinavir 400 mg and ritonavir 100 mg twice daily 

150 mg once daily 
darunavir 600 mg and ritonavir 100 mg twice daily 

fosamprenavir 700 mg and ritonavir 100 mg twice daily 

 
There are no data to recommend the use of Vitekta with dosing frequencies or HIV-1 protease 
inhibitors other than those presented in Table 1. 
 
Missed dose 
If the patient misses a dose of Vitekta within 18 hours of the time it is usually taken, the patient should 
take Vitekta with food as soon as possible and resume the normal dosing schedule.  If a patient misses 
a dose of Vitekta by more than 18 hours, and it is almost time for their next dose, the patient should 
not take the missed dose and simply resume the usual dosing schedule. 
 
If the patient vomits within 1 hour of taking Vitekta another tablet should be taken. 
 
Special populations 
 
Elderly 
No data are available on which to make a dose recommendation for patients over the age of 65 years 
(see section 5.2). 
 
Renal impairment 
No dose adjustment of Vitekta is required for patients with renal impairment (see section 5.2). 
 
Hepatic impairment 
No dose adjustment of Vitekta is required in patients with mild (Child-Pugh Class A) or moderate 
hepatic impairment (Child-Pugh Class B).  Elvitegravir has not been studied in patients with severe 
hepatic impairment (Child-Pugh Class C) (see sections 4.4 and 5.2). 
 
Paediatric population 
The safety and efficacy of elvitegravir in children aged 0 to less than 18 years have not yet been 
established (see section 5.1).  No data are available. 
 
Method of administration 
Vitekta should be taken orally, once daily with food (see section 5.2).  The film-coated tablet should 
not be chewed or crushed. 
 
4.3 Contraindications 
 
Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. 
 
Co-administration with the following medicinal products due to the potential for loss of virologic 
response and possible development of resistance (see section 4.5): 
• anticonvulsants: carbamazepine, phenobarbital, phenytoin 
• antimycobacterials: rifampicin 
• herbal products: St. John’s wort (Hypericum perforatum) 
 

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4.4 Special warnings and precautions for use 
 
General 
While effective viral suppression with antiretroviral therapy has been proven to substantially reduce 
the risk of sexual transmission, a residual risk cannot be excluded.  Precautions to prevent 
transmission should be taken in accordance with national guidelines. 
 
The use of Vitekta with HIV-1 protease inhibitors or dosing frequencies other than those presented in 
Table 1 may result in inadequate or elevated plasma levels of elvitegravir and/or the co-administered 
medicinal products. 
 
Resistance 
Elvitegravir-resistant viruses show cross-resistance to the integrase strand transfer inhibitor raltegravir 
in most cases (see section 5.1). 
 
Elvitegravir has a relatively low genetic barrier to resistance.  Therefore, whenever possible, Vitekta 
should be administered with a fully active ritonavir-boosted protease inhibitor and a second fully 
active antiretroviral agent to minimise the potential for virologic failure and the development of 
resistance (see section 5.1). 
 
Co-administration of other medicinal products 
Elvitegravir is primarily metabolised by CYP3A.  Co-administration of Vitekta with strong CYP3A 
inducers (including St. John’s wort [Hypericum perforatum], rifampicin, carbamazepine, 
phenobarbital and phenytoin) is contraindicated (see sections 4.3 and 4.5).  Co-administration of 
Vitekta with moderate CYP3A inducers (including, but not limited to, efavirenz and bosentan) is not 
recommended (see section 4.5). 
 
Due to the need for co-administration of Vitekta with a ritonavir-boosted protease inhibitor, 
prescribers should consult the Summary of Product Characteristics of the co-administered protease 
inhibitor and ritonavir for a description of contraindicated medicinal products and other significant 
drug-drug interactions that may cause potentially life-threatening adverse reactions or loss of 
therapeutic effect and possible development of resistance. 
 
Atazanavir/ritonavir and lopinavir/ritonavir have been shown to significantly increase the plasma 
concentrations of elvitegravir (see section 4.5).  When used in combination with atazanavir/ritonavir 
and lopinavir/ritonavir, the dose of Vitekta should be decreased from 150 mg once daily to 85 mg once 
daily (see section 4.2). 
 
Co-administration of Vitekta and related active substances: Vitekta must be used in combination with 
a ritonavir-boosted protease inhibitor.  Vitekta should not be used with a protease inhibitor boosted by 
another agent as dosing recommendations for such combinations have not been established.  Boosting 
elvitegravir with an agent other than ritonavir may result in suboptimal plasma concentrations of 
elvitegravir and/or the protease inhibitor leading to loss of therapeutic effect and possible development 
of resistance. 
 
Vitekta should not be used in combination with products containing elvitegravir or pharmacokinetic 
boosting agents other than ritonavir. 
 
Contraception requirements 
Female patients of childbearing potential should use either a hormonal contraceptive containing at 
least 30 µg ethinylestradiol and containing norgestimate as the progestagen or should use an 
alternative reliable method of contraception (see sections 4.5 and 4.6).  Co-administration of 
elvitegravir with oral contraceptives containing progestagens other than norgestimate have not been 
studied and, therefore, should be avoided. 
 
Patients using oestrogens as hormone replacement therapy should be clinically monitored for signs of 
oestrogen deficiency (see section 4.5). 

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Opportunistic infections 
Patients receiving Vitekta or any other antiretroviral therapy may continue to develop opportunistic 
infections and other complications of HIV infection, and therefore should remain under close clinical 
observation by physicians experienced in the treatment of patients with HIV associated diseases. 
 
Patients with HIV and hepatitis B or C virus co-infection 
Patients with chronic hepatitis B or C treated with antiretroviral therapy are at an increased risk for 
severe and potentially fatal hepatic adverse reactions. 
 
Physicians should refer to current HIV treatment guidelines for the optimal management of 
HIV infection in patients co-infected with hepatitis B virus (HBV). 
 
Liver disease 
Elvitegravir has not been studied in patients with severe hepatic impairment (Child-Pugh Class C).  No 
dose adjustment of Vitekta is required in patients with mild (Child-Pugh Class A) or moderate hepatic 
impairment (Child-Pugh Class B) (see sections 4.2 and 5.2). 
 
Patients with pre-existing liver dysfunction, including chronic active hepatitis, have an increased 
frequency of liver function abnormalities during combination antiretroviral therapy (CART) and 
should be monitored according to standard practice.  If there is evidence of worsening liver disease in 
such patients, interruption or discontinuation of treatment must be considered. 
 
Weight and metabolic parameters 
An increase in weight and in levels of blood lipids and glucose may occur during antiretroviral 
therapy.  Such changes may in part be linked to disease control and life style.  For lipids, there is in 
some cases evidence for a treatment effect, while for weight gain there is no strong evidence relating 
this to any particular treatment.  For monitoring of blood lipids and glucose reference is made to 
established HIV treatment guidelines.  Lipid disorders should be managed as clinically appropriate. 
 
Immune Reactivation Syndrome 
In HIV infected patients with severe immune deficiency at the time of institution of CART, an 
inflammatory reaction to asymptomatic or residual opportunistic pathogens may arise and cause 
serious clinical conditions, or aggravation of symptoms.  Typically, such reactions have been observed 
within the first few weeks or months of initiation of CART.  Relevant examples are cytomegalovirus 
retinitis, generalised and/or focal mycobacterial infections, and Pneumocystis jirovecii pneumonia.  
Any inflammatory symptoms should be evaluated and treatment instituted when necessary. 
 
Autoimmune disorders (such as Graves’ disease) have also been reported to occur in the setting of 
immune reactivation; however, the reported time to onset is more variable and these events can occur 
many months after initiation of treatment. 
 
Osteonecrosis 
Although the aetiology is considered to be multifactorial (including corticosteroid use, alcohol 
consumption, severe immunosuppression, higher body mass index), cases of osteonecrosis have been 
reported particularly in patients with advanced HIV disease and/or long-term exposure to CART.  
Patients should be advised to seek medical advice if they experience joint aches and pain, joint 
stiffness or difficulty in movement. 
 
Excipients 
Vitekta contains lactose.  Consequently, patients with rare hereditary problems of galactose 
intolerance, the Lapp lactase deficiency, or glucose-galactose malabsorption should not take this 
medicinal product. 
 
4.5 Interaction with other medicinal products and other forms of interaction 
 
Interaction studies have only been performed in adults. 

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Interactions with CYP3A inducers 
Elvitegravir is primarily metabolised by CYP3A (see section 5.2).  Medicinal products that are strong 
(causing a > 5-fold increase in substrate clearance) or moderate (causing a 2-5 fold increase in 
substrate clearance) inducers of CYP3A are expected to decrease plasma concentrations of 
elvitegravir. 
 
Concomitant use contraindicated 
Co-administration of Vitekta with medicinal products that are strong inducers of CYP3A is 
contraindicated as the expected decrease in plasma concentrations of elvitegravir can lead to loss of 
therapeutic effect and possible development of resistance to elvitegravir (see section 4.3). 
 
Concomitant use not recommended 
Co-administration of Vitekta with medicinal products that are moderate inducers of CYP3A 
(including, but not limited to, efavirenz and bosentan) is not recommended as the expected decrease in 
plasma concentrations of elvitegravir can lead to loss of therapeutic effect and possible development 
of resistance to elvitegravir (see section 4.4). 
 
Interactions requiring dose adjustment of Vitekta 
Elvitegravir undergoes oxidative metabolism by CYP3A (major route), and glucuronidation by 
UGT1A1/3 enzymes (minor route).  Co-administration of Vitekta with medicinal products that are 
potent inhibitors of UGT1A1/3 may result in increased elvitegravir plasma concentrations and dose 
modifications may be required.  For example, atazanavir/ritonavir and lopinavir/ritonavir (potent 
UGT1A1/3 inhibitors) have been shown to significantly increase the plasma concentrations of 
elvitegravir (see Table 2).  Accordingly, when used in combination with atazanavir/ritonavir and 
lopinavir/ritonavir, the dose of Vitekta should be decreased from 150 mg once daily to 85 mg once 
daily (see sections 4.2 and 4.4). 
 
Other interactions 
Elvitegravir is a modest inducer and may have the potential to induce CYP2C9 and/or inducible UGT 
enzymes.  As such, elvitegravir may decrease the plasma concentration of substrates of CYP2C9 (such 
as warfarin) or UGT (such as ethinyl estradiol).  In addition, in vitro studies have shown that 
elvitegravir is a weak to modest inducer of CYP1A2, CYP2C19 and CYP3A enzymes.  Elvitegravir 
would also have potential to be a weak to modest inducer of CYP2B6 and CYP2C8 enzymes, as these 
enzymes are regulated in a similar manner to CYP2C9 and CYP3A.  However, clinical data have 
shown there are no clinically relevant changes in the exposure of methadone (which is primarily 
metabolised by CYP2B6 and CYP2C19) following co-administration with boosted elvitegravir versus 
administration of methadone alone (see Table 2). 
 
Elvitegravir is a substrate for OATP1B1 and OATP1B3, and an inhibitor of OATP1B3 in vitro.  The 
in vivo relevance of these interactions is not clear. 
 
Interactions between elvitegravir and potential co-administered medicinal products are listed in 
Table 2 below (increase is indicated as “↑”, decrease as “↓”, no change as “↔”).  These interactions 
are based on either drug interaction studies or predicted interactions due to the expected magnitude of 
interaction and potential for serious adverse events or loss of therapeutic effect. 
 
Where interactions were studied, the effect on Vitekta was determined by comparing the 
pharmacokinetics of boosted elvitegravir (using either ritonavir or cobicistat as a pharmacokinetic 
enhancer) in the absence and presence of the co-administered medicinal product.  No interactions were 
studied using unboosted elvitegravir.  Except where indicated in Table 2, the dose of boosted 
elvitegravir or co-administered medicinal product was the same when administered alone or in 
combination.  The pharmacokinetic parameters of the protease inhibitors presented in Table 2 were 
assessed in the presence of ritonavir. 
 
Although there may be no actual or predicted interactions between a medicinal product and 
elvitegravir, there may be interactions between a medicinal product and ritonavir and/or the protease 

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inhibitor co-administered with elvitegravir.  The prescriber should always refer to the Summary of 
Product Characteristics for ritonavir, or the protease inhibitor. 
 
Table 2: Interactions between elvitegravir and other medicinal products 
 

Medicinal product by 
therapeutic areas 

Effects on drug levels 
Mean percent change in AUC, 

Cmax, Cmin 

Recommendation concerning 
co-administration with 

ritonavir-boosted elvitegravir 
ANTIRETROVIRALS 
HIV protease inhibitors 
Atazanavir (300 mg once daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (100 mg once daily) 

Atazanavir/Ritonavir has been 
shown to significantly increase 
the plasma concentrations of 
elvitegravir. 
 
Elvitegravir: 
AUC: ↑ 100% 
Cmax: ↑ 85% 
Cmin: ↑ 188% 
 
Atazanavir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↓ 35% 

When used in combination with 
atazanavir, the dose of Vitekta 
should be 85 mg once daily.  
When used in combination with 
Vitekta, the recommended dose of 
atazanavir is 300 mg with 
ritonavir 100 mg once daily. 
 
There are no data available to 
make dosing recommendations for 
co-administration with other doses 
of atazanavir (see section 4.2). 

Atazanavir (300 mg once daily) 
Elvitegravir (85 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔* 
Cmax: ↔* 
Cmin: ↑ 38%* 
 
Atazanavir: 
AUC: ↔** 
Cmax: ↔** 
Cmin: ↔** 
 
*when compared to 
elvitegravir/ritonavir 
150/100 mg once daily. 
 
**when compared to 
atazanavir/ritonavir 300/100 mg 
once daily. 

Darunavir (600 mg twice daily) 
Elvitegravir (125 mg once daily) 
Ritonavir (100 mg twice daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Darunavir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↓ 17% 

When used in combination with 
darunavir, the dose of Vitekta 
should be 150 mg once daily. 
 
There are no data available to 
make dosing recommendations for 
co-administration with other doses 
of darunavir (see section 4.2). 

Fosamprenavir (700 mg twice 
daily) 
Elvitegravir (125 mg once daily) 
Ritonavir (100 mg twice daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Fosamprenavir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

When used in combination with 
fosamprenavir, the dose of Vitekta 
should be 150 mg once daily. 
 
There are no data available to 
make dosing recommendations for 
co-administration with other doses 
of fosamprenavir (see section 4.2). 

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Medicinal product by 
therapeutic areas 

Effects on drug levels 
Mean percent change in AUC, 

Cmax, Cmin 

Recommendation concerning 
co-administration with 

ritonavir-boosted elvitegravir 
Lopinavir/Ritonavir (400/100 mg 
twice daily) 
Elvitegravir (125 mg once daily) 

Lopinavir/Ritonavir has been 
shown to significantly increase 
the plasma concentrations of 
elvitegravir. 
 
Elvitegravir: 
AUC: ↑ 75% 
Cmax: ↑ 52% 
Cmin: ↑ 138% 
 
Lopinavir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↓ 8% 

When used in combination with 
lopinavir/ritonavir, the dose of 
Vitekta should be 85 mg once 
daily. 
 
There are no data available to 
make dosing recommendations for 
co-administration with other doses 
of lopinavir/ritonavir (see 
section 4.2). 

Tipranavir (500 mg twice daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (200 mg twice daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Tipranavir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↓ 11% 

Due to insufficient clinical data, 
the combination of elvitegravir 
with tipranavir is not 
recommended (see section 4.2). 

NRTIs 
Didanosine (400 mg once daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Didanosine: 
AUC: ↓ 14% 
Cmax: ↓ 16% 

As didanosine is administered on 
an empty stomach, didanosine 
should be administered at least 
one hour before or two hours after 
Vitekta (which is administered 
with food).  Clinical monitoring is 
recommended. 

Zidovudine (300 mg twice daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Zidovudine: 
AUC: ↔ 
Cmax: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with zidovudine. 

Stavudine (40 mg once daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Stavudine: 
AUC: ↔ 
Cmax: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with stavudine. 

Abacavir (600 mg once daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Abacavir: 
AUC: ↔ 
Cmax: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with abacavir. Me

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Medicinal product by 
therapeutic areas 

Effects on drug levels 
Mean percent change in AUC, 

Cmax, Cmin 

Recommendation concerning 
co-administration with 

ritonavir-boosted elvitegravir 
Tenofovir disoproxil fumarate 
(300 mg once daily) 
Emtricitabine (200 mg once daily) 
Elvitegravir (50 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Tenofovir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Emtricitabine: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with tenofovir disoproxil fumarate 
or with emtricitabine. 

NNRTIs 
Efavirenz Interaction not studied with 

elvitegravir. 
 
Co-administration of efavirenz 
and elvitegravir is expected to 
decrease elvitegravir plasma 
concentrations which may result 
in loss of therapeutic effect and 
possible development of 
resistance. 

Co-administration is not 
recommended (see section 4.4). 

Etravirine (200 mg twice daily) 
Elvitegravir (150 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Etravirine: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with etravirine. 

Nevirapine Interaction not studied with 
elvitegravir. 
 
Co-administration of nevirapine 
and elvitegravir is expected to 
decrease elvitegravir plasma 
concentrations which may result 
in loss of therapeutic effect and 
possible development of 
resistance. 

Co-administration is not 
recommended (see section 4.4). 

Rilpivirine Interaction not studied with 
elvitegravir. 

Co-administration of elvitegravir 
and rilpivirine is not expected to 
change elvitegravir plasma 
concentrations, therefore no dose 
adjustment of Vitekta is required. 

CCR5 antagonists 
Maraviroc (150 mg twice daily) 
Elvitegravir (150 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Maraviroc:§ 
AUC: ↑ 186% 
Cmax: ↑ 115% 
Cmin: ↑ 323% 

No dose adjustment is required 
when Vitekta is co-administered 
with maraviroc. 
 
§Due to inhibition of CYP3A by 
ritonavir, maraviroc exposure is 
significantly increased. 

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Medicinal product by 
therapeutic areas 

Effects on drug levels 
Mean percent change in AUC, 

Cmax, Cmin 

Recommendation concerning 
co-administration with 

ritonavir-boosted elvitegravir 
ANTACIDS 
Magnesium/aluminum-containing 
antacid suspension (20 mL single 
dose) 
Elvitegravir (50 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir (antacid suspension 
given ± 4 hours from 
elvitegravir administration): 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Elvitegravir (simultaneous 
antacid administration): 
AUC: ↓ 45% 
Cmax: ↓ 47% 
Cmin: ↓ 41% 

Elvitegravir plasma concentrations 
are lower with antacids due to 
local complexation in the 
gastrointestinal tract and not to 
changes in gastric pH.  It is 
recommended to separate Vitekta 
and antacid administration by at 
least 4 hours. 

FOOD SUPPLEMENTS 
Multivitamin supplements Interaction not studied with 

elvitegravir. 
As the effect of cationic 
complexation of elvitegravir 
cannot be excluded when 
co-administered with multivitamin 
supplements, it is recommended to 
separate Vitekta and multivitamin 
supplements dosing by at least 
4 hours. 

NARCOTIC ANALGESICS 
Methadone (80-120 mg once daily) 
Elvitegravir (150 mg once daily) 
Cobicistat (150 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Methadone: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with methadone. 

Buprenorphine/Naloxone (16/4 mg 
to 24/6 mg daily) 
Elvitegravir (150 mg once daily) 
Cobicistat (150 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Buprenorphine: 
AUC: ↑ 35% 
Cmax: ↑ 12% 
Cmin: ↑ 66% 
 
Naloxone: 
AUC: ↓ 28% 
Cmax: ↓ 28% 

No dose adjustment is required 
when Vitekta is co-administered 
with buprenorphine/naloxone. 

ANTI-INFECTIVES 
Antifungals 
Ketoconazole (200 mg twice daily) 
Elvitegravir (150 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↑ 48% 
Cmax: ↔ 
Cmin: ↑ 67% 
 
↑ Ketoconazole§ 

No dose adjustment is required 
when Vitekta is co-administered 
with ketoconazole. 
 
§Due to inhibition of CYP3A by 
ritonavir, ketoconazole exposure is 
increased. 

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Medicinal product by 
therapeutic areas 

Effects on drug levels 
Mean percent change in AUC, 

Cmax, Cmin 

Recommendation concerning 
co-administration with 

ritonavir-boosted elvitegravir 
HCV protease inhibitors 
Telaprevir (750 mg three times 
daily)/ 
Elvitegravir (85 mg once daily) 
Atazanavir (300 mg once daily) 
Ritonavir (100 mg once daily) 

Telaprevir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↑ 40%* 
 
*Compared to 
atazanavir/ritonavir 300/100 mg 
plus elvitegravir 85 mg once 
daily. 

No dose adjustment is required 
when Vitekta is co-administered 
with ritonavir-boosted atazanavir 
plus telaprevir. 

Antimycobacterials 
Rifabutin (150 mg once every 
other day) 
Elvitegravir (300 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔* 
Cmax: ↔* 
Cmin: ↔* 
 
Rifabutin: 
AUC: ↔** 
Cmax: ↔** 
Cmin: ↔** 

Co-administration of Vitekta and 
rifabutin is not recommended.  If 
the combination is needed, the 
recommended dose of rifabutin is 
150 mg 3 times per week on set 
days (for example Monday-
Wednesday-Friday). 
 
No dose adjustment of Vitekta is 
required when co-administered 
with reduced dose of rifabutin. 
 
Further dose reduction of rifabutin 
has not been studied.  It should be 
kept in mind that a twice weekly 
dose of 150 mg may not provide 
an optimal exposure to rifabutin 
thus leading to a risk of rifamycin 
resistance and a treatment failure. 
 
§Due to inhibition of CYP3A by 
ritonavir, 25-O-desacetyl-rifabutin 
exposure is increased. 

 25-O-desacetyl-rifabutin:§ 
AUC: ↑ 851%** 
Cmax: ↑ 440%** 
Cmin: ↑ 1,836%** 
 
*when compared to 
elvitegravir/ritonavir 
300/100 mg once daily. 
 
**when compared to rifabutin 
300 mg once daily. 
 
Total antimycobacterial activity 
was increased by 50%. 

ANTICOAGULANTS 
Warfarin Interaction not studied with 

elvitegravir. 
 
Concentrations of warfarin may 
be affected upon 
co-administration with 
elvitegravir. 

It is recommended that the 
international normalised ratio 
(INR) be monitored upon 
co-administration of Vitekta.  INR 
should continue to be monitored 
during the first weeks following 
cessation of treatment with 
Vitekta. 

H2-RECEPTOR ANTAGONISTS 
Famotidine (40 mg once daily) 
Elvitegravir (150 mg once daily) 
Cobicistat (150 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with famotidine. 

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Medicinal product by 
therapeutic areas 

Effects on drug levels 
Mean percent change in AUC, 

Cmax, Cmin 

Recommendation concerning 
co-administration with 

ritonavir-boosted elvitegravir 
HMG-CoA REDUCTASE INHIBITORS 
Rosuvastatin (10 mg single dose) 
Elvitegravir (150 mg once daily) 
Cobicistat (150 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Rosuvastatin: 
AUC: ↑ 38% 
Cmax: ↑ 89% 
Cmin: ↑ 43% 

No dose adjustment is required 
when Vitekta is co-administered 
with rosuvastatin. 

Atorvastatin 
Fluvastatin 
Pitavastatin 
Pravastatin 

Interaction not studied with 
elvitegravir. 
 
Plasma concentrations of OATP 
substrates are not expected to 
change upon co-administration 
of elvitegravir. 
 
Plasma concentrations of 
elvitegravir are not expected to 
change upon co-administration 
of OATP substrates/inhibitors. 

No dose adjustment is required 
when Vitekta is co-administered 
with atorvastatin, fluvastatin, 
pitavastatin or pravastatin. 

ORAL CONTRACEPTIVES 
Norgestimate (0.180/0.215 mg 
once daily) 
Ethinylestradiol (0.025 mg once 
daily) 
Elvitegravir (150 mg once daily) 
Cobicistat (150 mg once daily)1 
 

Norgestimate: 
AUC: ↑ 126% 
Cmax: ↑ 108% 
Cmin: ↑ 167% 
 
Ethinylestradiol: 
AUC: ↓ 25% 
Cmax: ↔ 
Cmin: ↓ 44% 
 
Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

Caution should be exercised when 
co-administering Vitekta and a 
hormonal contraceptive.  The 
hormonal contraceptive should 
contain at least 30 µg 
ethinylestradiol and contain 
norgestimate as the progestagen or 
patients should use an alternative 
reliable method of contraception 
(see sections 4.4 and 4.6). 
 
The long-term effects of 
substantial increases in 
progesterone exposure are 
unknown.  Co-administration of 
elvitegravir with oral 
contraceptives containing 
progestagens other than 
norgestimate has not been studied 
and therefore should be avoided. 

PROTON PUMP INHIBITORS 
Omeprazole (40 mg once daily) 
Elvitegravir (50 mg once daily 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with omeprazole. 

1 This study was conducted using the fixed-dose combination tablet elvitegravir/cobicistat/emtricitabine/tenofovir 
disoproxil. 

 
4.6 Fertility, pregnancy and lactation 
 
Women of childbearing potential / contraception in males and females 
The use of Vitekta must be accompanied by the use of effective contraception (see sections 4.4 
and 4.5). 
 
Pregnancy 
There are no or limited clinical data with elvitegravir in pregnant women. 

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Animal studies do not indicate direct or indirect harmful effects of elvitegravir with respect to 
reproductive toxicity.  However, the maximum exposures evaluated in the rabbit were not in excess of 
those achieved therapeutically (see section 5.3). 
 
Vitekta should not be used during pregnancy unless the clinical condition of the woman requires 
treatment with elvitegravir. 
 
Breast-feeding 
It is unknown whether elvitegravir/metabolites are excreted in human milk.  Available 
pharmacodynamic/toxicological data in rats have shown excretion of elvitegravir in milk.  A risk to 
the newborns/infants cannot be excluded.  Therefore, Vitekta should not be used during breast-
feeding. 
 
In order to avoid transmission of HIV to the infant it is recommended that HIV infected women do not 
breast-feed their infants under any circumstances. 
 
Fertility 
No human data on the effect of elvitegravir on fertility are available.  Animal studies do not indicate 
harmful effects of elvitegravir on fertility. 
 
4.7 Effects on ability to drive and use machines 
 
No studies on the effects of elvitegravir on the ability to drive and use machines have been performed. 
 
4.8 Undesirable effects 
 
Summary of the safety profile 
Assessment of adverse reactions is based on data from a controlled clinical study (GS-US-183-0145) 
in which 712 HIV-1 infected, antiretroviral treatment-experienced adults received elvitegravir 
(n = 354) or raltegravir (n = 358) each administered with a background regimen consisting of a fully 
active ritonavir-boosted protease inhibitor and other antiretroviral agents.  Of these 712 patients, 543 
(269 elvitegravir and 274 raltegravir) and 439 (224 elvitegravir and 215 raltegravir) received at least 
48 and 96 weeks of treatment, respectively. 
 
The most frequently reported adverse reactions to elvitegravir were diarrhoea (7.1%) and nausea 
(4.0%) (see Table 3). 
 
Tabulated summary of adverse reactions 
Adverse reactions to elvitegravir from clinical study experience are listed in Table 3 below, by body 
system organ class and frequency.  Within each frequency grouping, undesirable effects are presented 
in order of decreasing seriousness.  Frequencies are defined as common (≥ 1/100 to < 1/10) or 
uncommon (≥ 1/1,000 to < 1/100). 
 

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Table 3: Tabulated summary of adverse reactions to elvitegravir based on experience for 
96 weeks from clinical study GS-US-183-0145 
 
Frequency Adverse reaction 
Psychiatric disorders: 

Uncommon suicidal ideation and suicide attempt (in patients with a pre-existing history of depression or psychiatric illness), depression, insomnia 
Nervous system disorders: 
Common headache 
Uncommon dizziness, paraesthesia, somnolence, dysgeusia 
Gastrointestinal disorders: 
Common abdominal pain, diarrhoea, vomiting, nausea 
Uncommon dyspepsia, abdominal distension, flatulence 
Skin and subcutaneous tissue disorders: 
Common rash 
General disorders and administration site conditions: 
Common fatigue 
 
Description of selected adverse reactions 
 
Metabolic parameters 
Weight and levels of blood lipids and glucose may increase during antiretroviral therapy (see 
section 4.4). 
 
Immune Reactivation Syndrome 
In HIV infected patients with severe immune deficiency at the time of initiation of CART, an 
inflammatory reaction to asymptomatic or residual opportunistic infections may arise.  Autoimmune 
disorders (such as Graves’ disease) have also been reported; however, the reported time to onset is 
more variable and these events can occur many months after initiation of treatment (see section 4.4). 
 
Osteonecrosis 
Cases of osteonecrosis have been reported, particularly in patients with generally acknowledged risk 
factors, advanced HIV disease or long-term exposure to CART.  The frequency of this is unknown 
(see section 4.4). 
 
Diarrhoea 
In study GS-US-183-0145, diarrhoea was reported as an adverse reaction in 7.1% of subjects in the 
elvitegravir group and in 5.3% of subjects in the raltegravir group.  In these subjects, diarrhoea was 
mild to moderate in severity and did not result in discontinuation of study drug. 
 
Paediatric population 
No data are available for children below 18 years of age.  Vitekta is not recommended in this 
population (see section 4.2). 
 
Reporting of suspected adverse reactions 
Reporting suspected adverse reactions after authorisation of the medicinal product is important.  It 
allows continued monitoring of the benefit/risk balance of the medicinal product.  Healthcare 
professionals are asked to report any suspected adverse reactions via the national reporting system 
listed in Appendix V. 
 
4.9 Overdose 
 
If overdose occurs the patient must be monitored for evidence of toxicity.  Treatment of overdose with 
elvitegravir consists of general supportive measures including monitoring of vital signs as well as 
observation of the clinical status of the patient. 
 

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15 

There is no specific antidote for overdose with elvitegravir.  As elvitegravir is highly bound to plasma 
proteins, it is unlikely that it will be significantly removed by haemodialysis or peritoneal dialysis. 
 
 
5. PHARMACOLOGICAL PROPERTIES 
 
5.1 Pharmacodynamic properties 
 
Pharmacotherapeutic group: Antivirals for systemic use, other antivirals, ATC code: J05AX11. 
 
Mechanism of action and pharmacodynamic effects 
Elvitegravir is an HIV-1 integrase strand transfer inhibitor (INSTI).  Integrase is an HIV-1 encoded 
enzyme that is required for viral replication.  Inhibition of integrase prevents the integration of 
HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation 
of the viral infection.  Elvitegravir does not inhibit human topoisomerases I or II. 
 
Antiviral activity in vitro 
The antiviral activity of elvitegravir against laboratory and clinical isolates of HIV-1 was assessed in 
lymphoblastoid cells, monocyte/macrophage cells, and peripheral blood lymphocytes and the 50% 
effective concentration (EC50) values were in the range of 0.02 to 1.7 nM.  Elvitegravir displayed 
antiviral activity in cell culture against HIV-1 clades A, B, C, D, E, F, G, and O (EC50 values ranged 
from 0.1 to 1.3 nM) and activity against HIV-2 (EC50 of 0.53 nM).  The in vitro antiviral activity of 
elvitegravir when combined with antiretroviral drugs from the nucleos(t)ide reverse transcriptase 
inhibitor (NRTI), non-nucleoside reverse transcriptase inhibitor (NNRTI), protease inhibitor (PI), 
integrase strand transfer inhibitor, fusion inhibitor, or CCR5 co-receptor antagonist classes showed no 
antagonism. 
 
Elvitegravir did not show inhibition of replication of HBV or HCV in vitro. 
 
Resistance 
In cell culture 
HIV-1 isolates with reduced susceptibility to elvitegravir have been selected in cell culture.  
Phenotypic resistance to elvitegravir was most commonly associated with the primary integrase 
substitutions T66I, E92Q and Q148R.  Additional integrase substitutions observed in cell culture 
selection included H51Y, F121Y, S147G, S153Y, E157Q, and R263K. 
 
Cross resistance 
Elvitegravir-resistant viruses show varying degrees of cross-resistance to the integrase strand transfer 
inhibitor raltegravir depending on the type and number of substitutions.  Viruses expressing the 
T66I/A substitutions maintain susceptibility to raltegravir, while most other patterns of 
elvitegravir-associated substitutions are associated with reduced susceptibility to raltegravir.  With the 
exception of Y143C/R/H, HIV-1 with the primary raltegravir-associated substitutions T66K, 
Q148H/K/R, or N155H in integrase is associated with reduced susceptibility to elvitegravir. 
 
In treatment-experienced patients 
In an analysis of HIV-1 isolates from treatment-failure subjects in study GS-US-183-0145 through 
week 96, the development of one or more primary elvitegravir resistance-associated substitutions was 
observed in 23 of the 86 subjects with evaluable genotypic data from paired baseline and elvitegravir 
treatment-failure isolates (23/351 elvitegravir-treated subjects, 6.6%).  Similar rates of raltegravir 
resistance development occurred in the HIV-1 from subjects treated with raltegravir (26/351 
raltegravir-treated subjects, 7.4%).  The most common substitutions that emerged in HIV-1 isolates 
from elvitegravir-treated subjects were T66I/A (n = 8), E92Q/G (n = 7), T97A (n = 4), S147G (n = 4), 
Q148R (n = 4), and N155H (n = 5) in integrase.  In phenotypic analyses of HIV-1 isolates with 
resistance substitutions from elvitegravir-treated subjects, 14/20 (70%) had reduced susceptibility to 
elvitegravir and 12/20 (60%) had reduced susceptibility to raltegravir. 
 

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Clinical experience 
In treatment-experienced HIV-1 infected patients 
The efficacy of elvitegravir is primarily based on the analyses through 96 weeks from one randomised, 
double-blind, active-controlled study, study GS-US-183-0145, in treatment-experienced, 
HIV-1 infected patients (n = 702). 
 
In study GS-US-183-0145, patients were randomised in a 1:1 ratio to receive either elvitegravir 
(150 mg or 85 mg) once daily or raltegravir 400 mg twice daily, each administered with a background 
regimen (BR) containing a fully-active ritonavir-boosted protease inhibitor (either atazanavir, 
darunavir, fosamprenavir, lopinavir or tipranavir) and a second agent.  The BR was selected by the 
investigator based on genotypic/phenotypic resistance testing and prior antiretroviral treatment history.  
Randomisation was stratified by screening HIV-1 RNA level (≤ 100,000 copies/mL or 
> 100,000 copies/mL) and the class of the second agent (NRTI or other classes).  Virologic response 
rate was evaluated in both treatment arms.  Virologic response was defined as achieving an 
undetectable viral load (HIV-1 RNA < 50 copies/mL). 
 
Baseline characteristics and treatment outcomes through 96 weeks for study GS-US-183-0145 are 
presented in Tables 4 and 5 respectively. 
 
Table 4: Demographic and baseline disease characteristics of antiretroviral treatment-
experienced HIV-1 infected adult subjects in study GS-US-183-0145 
 
 
 

Elvitegravir + background 
regimen 
n = 351 

Raltegravir + background 
regimen 
n = 351 

Demographic characteristics 
Median age, years (min-max) 44 

(20-78) 
45 

(19-74) 
Sex   
 Male 83.2% 80.9% 
 Female 16.8% 19.1% 
Ethnicity   
 White 60.1% 64.4% 
 Black/African American 35.6% 32.2% 
 Asian 2.6% 1.4% 
 Other 1.7% 2.0% 
Baseline disease characteristics 
Median baseline plasma 
HIV-1 RNA (range) 
log10 copies/mL 

4.35 
(1.69-6.63) 

4.42 
(1.69-6.10) 

Percentage of subjects with 
viral load > 100,000 copies/mL 

25.6 25.6 

Median baseline CD4+ cell 
count (range), cells/mm3 

227.0 
(2.0-1,374.0) 

215.0 
(1.0-1,497.0) 

Percentage of subjects with 
CD4+ cell counts 
≤ 200 cells/mm3 

44.4 
 

44.9 

Baseline genotypic sensitivity 
scorea 

0 
1 
2 
3 

 
 

1% 
14% 
81% 
3% 

 
 

< 1% 
15% 
83% 
2% 

a Genotypic sensitivity scores are calculated by summing up drug susceptibility values (1 = sensitive; 0 = reduced 
susceptibility) on all drugs in the baseline background regimen. 

 

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Table 5: Virologic outcome of randomised treatment of study GS-US-183-0145 at week 48 and 
week 96 (snapshot analysis)a 
 
 Week 48 Week 96 
 Elvitegravir 

+ background 
regimen 
n = 351 

Raltegravir 
+ background 

regimen 
n = 351 

Elvitegravir 
+ background 

regimen 
n = 351 

Raltegravir 
+ background 

regimen 
n = 351 

Virologic success 
HIV-1 RNA 
< 50 copies/mL 

60% 58% 52% 53% 

Treatment difference 2.2% (95% CI = -5.0%, 9.3%) -0.5% (95% CI = -7.9%, 6.8%) 
Virologic failureb 33% 32% 36% 31% 
No virologic data at 
week 48 or week 96 
window 

7% 11% 12% 16% 

Discontinued study drug 
due to AE or deathc 

2% 5% 3% 7% 

Discontinued study drug 
due to other reasons and 
last available 
HIV-1 RNA 
< 50 copies/mLd 

4% 5% 8% 9% 

Missing data during 
window but on study 
drug 

1% 1% 1% 1% 

a Week 48 window is between day 309 and 364 (inclusive), week 96 window is between day 645 and 700 (inclusive). 
b Includes subjects who had ≥ 50 copies/mL in the week 48 or week 96 window, subjects who discontinued early due to 

lack or loss of efficacy, subjects who had a viral load ≥ 50 copies/mL at time of change in background regimen, subjects 
who discontinued for reasons other than an adverse event (AE), death or lack or loss of efficacy and at the time of 
discontinuation had a viral load of ≥ 50 copies/mL. 

c Includes patients who discontinued due to an AE or death at any time point from day 1 through the time window if this 
resulted in no virologic data on treatment during the specified window. 

d Includes subjects who discontinued for reasons other than an AE, death or lack or loss of efficacy, e.g., withdrew consent, 
loss to follow-up, etc. 

 
Elvitegravir was non-inferior in achieving HIV-1 RNA < 50 copies/mL when compared to raltegravir. 
 
Among subjects with a genotypic sensitivity score of ≤ 1, 76% and 69% had HIV-1 RNA 
< 50 copies/mL at week 48 in the elvitegravir and raltegravir treatment arms, respectively.  Among 
subjects with a genotypic sensitivity score > 1, 57% and 56% had HIV-1 RNA < 50 copies/mL at 
week 48 in the elvitegravir and raltegravir treatment arms, respectively. 
 
In study GS-US-183-0145, the mean increase from baseline in CD4+ cell count at week 96 was 
205 cells/mm3 in the elvitegravir-treated patients and 198 cells/mm3 in the raltegravir-treated patients. 
 
In study GS-US-183-0145, subgroup analyses by co-administered protease inhibitor showed similar 
rates of virologic success for elvitegravir and raltegravir within each protease inhibitor subgroup at 
weeks 48 and 96 (HIV-1 RNA < 50 copies/mL) (Table 6). 
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Table 6: Virologic success by co-administered protease inhibitor in study GS-US-183-0145 at 
week 48 and week 96 (snapshot analysis) 
 
  Elvitegravir versus 

raltegravir 
HIV-1 RNA 
< 50 copies/mL, n/N (%) 

Elvitegravir 
(N = 351) 

Raltegravir 
(N = 351) 

Difference in percentages 
(95% CI)a 

Virologic success at 
week 48 

   

Darunavir/ritonavir 126/202 (62.4%) 122/207 (58.9%) 3.4% (-6.0% to 12.9%) 
Lopinavir/ritonavir 39/68 (57.4%) 37/68 (54.4%) 2.9% (-13.7% to 19.6%) 
Atazanavir/ritonavir 34/61 (55.7%) 28/51 (54.9%) 0.8% (-17.7% to 19.3%) 
Fosamprenavir/ritonavir 8/14 (57.1%) 10/18 (55.6%) 1.6% (-33.0% to 36.2%) 
Tipranavir/ritonavir 3/6 (50.0%) 5/7 (71.4%) -21.4% (-73.6% to 30.7%) 

Virologic success at 
week 96 

   

Darunavir/ritonavir 105/202 (52.0%) 112/207 (54.1%) -2.1% (-11.8% to 7.5%) 
Lopinavir/ritonavir 36/68 (52.9%) 37/68 (54.4%) -1.5% (-18.2% to 15.3%) 
Atazanavir/ritonavir 33/61 (54.1%) 23/51 (45.1%) 9.0% (-9.5% to 27.5%) 
Fosamprenavir/ritonavir 7/14 (50.0%) 11/18 (61.1%) -11.1% (-45.7% to 23.4%) 
Tipranavir/ritonavir 3/6 (50.0%) 3/7 (42.9%) 7.1% (-47.1% to 61.4%) 

a The difference in proportions and its 95% CIs between randomised treatment groups is based on normal approximation. 
 
Although limited by the small number of female subjects in study GS-US-183-0145, subgroup 
analysis by gender showed that the rates of virologic success in female subjects at weeks 48 and 96 
(HIV-1 RNA < 50 copies/mL) were numerically lower in the elvitegravir treatment arm than in the 
raltegravir treatment arm.  Virologic success rates at week 48 for elvitegravir and raltegravir were 
47.5% (28/59) and 62.7% (42/67) (difference: -12.3% [95% CI: -30.1% to 5.5%]), respectively, for 
female subjects, and 62.3% (182/292) and 56.3% (160/284) (difference: 5.3% [95% CI: -2.5% to 
13.2%]), respectively, for male subjects.  Virologic success rates at week 96 for elvitegravir and 
raltegravir were 39.0% (23/59) and 52.2% (35/67) (difference: -8.4% [95% CI: -26.1% to 9.2%]), 
respectively, for female subjects, and 55.1% (161/292) and 53.2% (151/284) (difference: 1.5% 
[95% CI: -6.5% to 9.6%]), respectively, for male subjects. 
 
Paediatric population 
The European Medicines Agency has deferred the obligation to submit the results of studies with 
elvitegravir in one or more subsets of the paediatric population in the treatment of HIV-1 infection 
(see section 4.2 for information on paediatric use). 
 
5.2 Pharmacokinetic properties 
 
Absorption 
Following oral administration of ritonavir-boosted elvitegravir with food in HIV-1 infected subjects, 
elvitegravir peak plasma concentrations were observed 4 hours post-dose.  The steady-state mean Cmax, 
AUCtau, and Ctrough (mean ± SD) following multiple doses of elvitegravir plus a ritonavir-boosted 
protease inhibitor (150 mg elvitegravir with darunavir or fosamprenavir; 85 mg elvitegravir with 
atazanavir or lopinavir) in HIV-1 infected subjects were 1.4 ± 0.39 μg/mL, 18 ± 6.8 μg•h/mL, and 
0.38 ± 0.22 μg/mL for elvitegravir, respectively.  The absolute oral bioavailability has not been 
determined. 
 
Relative to fasting conditions, the administration of boosted elvitegravir as the fixed-dose combination 
150 mg elvitegravir/150 mg cobicistat/200 mg emtricitabine/245 mg tenofovir disoproxil with a light 
meal (approximately 373 kcal, 20% fat) or high-fat meal (approximately 800 kcal, 50% fat) resulted in 
increased exposures of elvitegravir.  The Cmax and AUCtau of elvitegravir increased 22% and 36% with 
a light meal, while increasing 56% and 91% with a high-fat meal, respectively. 
 

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Distribution 
Elvitegravir is 98-99% bound to human plasma proteins and the binding is independent of drug 
concentration over the range of 1.0 ng/mL to 1.6 µg/mL.  The mean plasma to blood drug 
concentration ratio is 1.37. 
 
Biotransformation 
Elvitegravir undergoes oxidative metabolism by CYP3A (major route), and glucuronidation via 
UGT1A1/3 enzymes (minor route). 
 
Ritonavir inhibits CYP3A, thereby substantially increasing the plasma concentrations of elvitegravir.  
Administration of once-daily ritonavir (20-200 mg) results in an increased elvitegravir exposure 
following repeat once-daily administration, with elvitegravir exposure reaching a plateau with 
approximately 100 mg of ritonavir.  Further increases in ritonavir dose do not result in further 
increases in elvitegravir exposure.  Vitekta is indicated for use only when co-administered with 
ritonavir as a boosting agent. 
 
Mean steady-state exposure (AUCtau) of unboosted elvitegravir is ~ 20% lower after multiple dosing 
versus a single dose, indicating modest autoinduction of its metabolism.  Upon boosting with ritonavir 
(100 mg), net inhibition of elvitegravir metabolism is observed with significantly increased systemic 
exposures (20-fold higher AUC), high trough concentrations, and longer median elimination half-life 
(9.5 versus 3.5 hours). 
 
Following oral administration of a single dose of ritonavir-boosted [14C]elvitegravir, elvitegravir was 
the predominant species in plasma, representing approximately 94% and 61% of the circulating 
radioactivity at 32 and 48 hours, respectively.  Metabolites produced by aromatic and aliphatic 
hydroxylation or glucuronidation are present in very low levels and do not contribute to the overall 
antiviral activity of elvitegravir. 
 
Elimination 
Following oral administration of ritonavir-boosted [14C]elvitegravir, 94.8% of the dose was recovered 
in faeces, consistent with the hepatobiliary elimination of elvitegravir; 6.7% of the administered dose 
was recovered in urine as metabolites.  The median terminal plasma half-life of ritonavir-boosted 
elvitegravir is approximately 8.7 to 13.7 hours. 
 
Linearity/non-linearity 
Elvitegravir plasma exposures are non-linear and less than dose-proportional, likely due to solubility-
limited absorption. 
 
Elderly 
Pharmacokinetics of elvitegravir have not been fully evaluated in the elderly (over 65 years of age). 
 
Gender 
No clinically relevant pharmacokinetic differences due to gender have been identified for boosted 
elvitegravir. 
 
Ethnicity 
No clinically relevant pharmacokinetic differences due to ethnicity have been identified for boosted 
elvitegravir. 
 
Paediatric population 
The pharmacokinetics of elvitegravir in paediatric subjects have not been established. 
 
Renal impairment 
A study of the pharmacokinetics of boosted elvitegravir was performed in non HIV-1 infected subjects 
with severe renal impairment (estimated creatinine clearance below 30 mL/min).  No clinically 
relevant differences in elvitegravir pharmacokinetics were observed between subjects with severe 

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renal impairment and healthy subjects.  No dose adjustment of Vitekta is required for patients with 
renal impairment. 
 
Hepatic impairment 
Elvitegravir is primarily metabolised and eliminated by the liver.  A study of the pharmacokinetics of 
boosted elvitegravir was performed in non-HIV-1 infected subjects with moderate hepatic impairment 
(Child-Pugh Class B).  No clinically relevant differences in elvitegravir pharmacokinetics were 
observed between subjects with moderate impairment and healthy subjects.  No dose adjustment of 
Vitekta is necessary for patients with mild to moderate hepatic impairment.  The effect of severe 
hepatic impairment (Child-Pugh Class C) on the pharmacokinetics of elvitegravir has not been studied. 
 
Hepatitis B and/or hepatitis C virus co-infection 
Limited data from population pharmacokinetic analysis (n = 56) indicated that hepatitis B and/or 
C virus infection had no clinically relevant effect on the exposure of boosted elvitegravir. 
 
5.3 Preclinical safety data 
 
Non-clinical data reveal no special hazard for humans based on conventional studies of safety 
pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, toxicity to reproduction 
and development.  The maximum doses of elvitegravir tested in the development toxicity studies in 
rats and rabbits corresponded to exposures that are approximately 29-fold and 0.2-fold the human 
therapeutic exposure, respectively. 
 
Elvitegravir was negative in an in vitro bacterial mutagenicity test (Ames test) and negative in an 
in vivo rat micronucleus assay at doses up to 2,000 mg/kg.  In an in vitro chromosomal aberration test, 
elvitegravir was negative with metabolic activation; however, an equivocal response was observed 
without activation. 
 
Elvitegravir did not show any carcinogenic potential in long-term oral carcinogenicity studies in mice 
and rats. 
 
The active substance elvitegravir is persistent in the environment. 
 
 
6. PHARMACEUTICAL PARTICULARS 
 
6.1 List of excipients 
 
Tablet core 
Croscarmellose sodium 
Hydroxypropyl cellulose 
Lactose monohydrate 
Magnesium stearate 
Microcrystalline cellulose 
Sodium lauryl sulfate 
 
Film-coating 
Indigo carmine aluminium lake (E132) 
Macrogol 3350 (E1521) 
Polyvinyl alcohol (partially hydrolysed) (E1203) 
Talc (E553B) 
Titanium dioxide (E171) 
Iron oxide yellow (E172) 
 
6.2 Incompatibilities 
 
Not applicable. 

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6.3 Shelf life 
 
4 years. 
 
6.4 Special precautions for storage 
 
This medicinal product does not require any special storage conditions. 
 
6.5 Nature and contents of container 
 
High density polyethylene (HDPE) bottle with a child-resistant closure containing 30 film-coated 
tablets. 
 
Pack size: 1 bottle of 30 film-coated tablets. 
 
6.6 Special precautions for disposal 
 
Any unused medicinal product or waste material should be disposed of in accordance with local 
requirements. 
 
 
7. MARKETING AUTHORISATION HOLDER 
 
Gilead Sciences International Limited 
Cambridge 
CB21 6GT 
United Kingdom 
 
 
8. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/13/883/001 
 
 
9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION 
 
Date of first authorisation: 13 November 2013 
 
 
10. DATE OF REVISION OF THE TEXT 
 
 
Detailed information on this medicinal product is available on the website of the European Medicines 
Agency http://www.ema.europa.eu. 

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This medicinal product is subject to additional monitoring.  This will allow quick identification of 
new safety information.  Healthcare professionals are asked to report any suspected adverse reactions.  
See section 4.8 for how to report adverse reactions. 
 
1. NAME OF THE MEDICINAL PRODUCT 
 
Vitekta 150 mg film-coated tablets 
 
 
2. QUALITATIVE AND QUANTITATIVE COMPOSITION 
 
Each film-coated tablet contains 150 mg of elvitegravir. 
 
Excipient with known effect: Each tablet contains 10.9 mg lactose (as monohydrate). 
 
For the full list of excipients, see section 6.1. 
 
 
3. PHARMACEUTICAL FORM 
 
Film-coated tablet (tablet). 
 
Green, triangle-shaped, film-coated tablet of dimensions 10.9 mm x 10.5 mm, debossed with “GSI” on 
one side of the tablet and “150” on the other side of the tablet. 
 
 
4. CLINICAL PARTICULARS 
 
4.1 Therapeutic indications 
 
Vitekta co-administered with a ritonavir-boosted protease inhibitor and with other antiretroviral 
agents, is indicated for the treatment of human immunodeficiency virus-1 (HIV-1) infection in adults 
who are infected with HIV-1 without known mutations associated with resistance to elvitegravir (see 
sections 4.2 and 5.1). 
 
4.2 Posology and method of administration 
 
Therapy should be initiated by a physician experienced in the management of HIV infection. 
 
Posology 
Vitekta must be administered in combination with a ritonavir-boosted protease inhibitor. 
 
The Summary of Product Characteristics for the co-administered ritonavir-boosted protease inhibitor 
should be consulted. 
 
The recommended dose of Vitekta is one 85 mg tablet or one 150 mg tablet taken orally once daily 
with food.  The choice of dose of Vitekta depends on the co-administered protease inhibitor (see 
Table 1 and sections 4.4 and 4.5).  For use of the 85 mg tablet, please refer to the Summary of Product 
Characteristics for Vitekta 85 mg tablets. 
 
Vitekta should be administered once daily as follows: 
- Either at the same time as a once daily ritonavir-boosted protease inhibitor 
- Or with the first dose of a twice daily ritonavir-boosted protease inhibitor. 
 

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Table 1: Recommended dosing regimens 
 
Dose of Vitekta Dose of co-administered ritonavir-boosted protease inhibitor 

85 mg once daily 
atazanavir 300 mg and ritonavir 100 mg once daily 

lopinavir 400 mg and ritonavir 100 mg twice daily 

150 mg once daily 
darunavir 600 mg and ritonavir 100 mg twice daily 

fosamprenavir 700 mg and ritonavir 100 mg twice daily 

 
There are no data to recommend the use of Vitekta with dosing frequencies or HIV-1 protease 
inhibitors other than those presented in Table 1. 
 
Missed dose 
If the patient misses a dose of Vitekta within 18 hours of the time it is usually taken, the patient should 
take Vitekta with food as soon as possible and resume the normal dosing schedule.  If a patient misses 
a dose of Vitekta by more than 18 hours, and it is almost time for their next dose, the patient should 
not take the missed dose and simply resume the usual dosing schedule. 
 
If the patient vomits within 1 hour of taking Vitekta another tablet should be taken. 
 
Special populations 
 
Elderly 
No data are available on which to make a dose recommendation for patients over the age of 65 years 
(see section 5.2). 
 
Renal impairment 
No dose adjustment of Vitekta is required for patients with renal impairment (see section 5.2). 
 
Hepatic impairment 
No dose adjustment of Vitekta is required in patients with mild (Child-Pugh Class A) or moderate 
hepatic impairment (Child-Pugh Class B).  Elvitegravir has not been studied in patients with severe 
hepatic impairment (Child-Pugh Class C) (see sections 4.4 and 5.2). 
 
Paediatric population 
The safety and efficacy of elvitegravir in children aged 0 to less than 18 years have not yet been 
established (see section 5.1).  No data are available. 
 
Method of administration 
Vitekta should be taken orally, once daily with food (see section 5.2).  The film-coated tablet should 
not be chewed or crushed. 
 
4.3 Contraindications 
 
Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. 
 
Co-administration with the following medicinal products due to the potential for loss of virologic 
response and possible development of resistance (see section 4.5): 
• anticonvulsants: carbamazepine, phenobarbital, phenytoin 
• antimycobacterials: rifampicin 
• herbal products: St. John’s wort (Hypericum perforatum) 
 

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4.4 Special warnings and precautions for use 
 
General 
While effective viral suppression with antiretroviral therapy has been proven to substantially reduce 
the risk of sexual transmission, a residual risk cannot be excluded.  Precautions to prevent 
transmission should be taken in accordance with national guidelines. 
 
The use of Vitekta with HIV-1 protease inhibitors or dosing frequencies other than those presented in 
Table 1 may result in inadequate or elevated plasma levels of elvitegravir and/or the co-administered 
medicinal products. 
 
Resistance 
Elvitegravir-resistant viruses show cross-resistance to the integrase strand transfer inhibitor raltegravir 
in most cases (see section 5.1). 
 
Elvitegravir has a relatively low genetic barrier to resistance.  Therefore, whenever possible, Vitekta 
should be administered with a fully active ritonavir-boosted protease inhibitor and a second fully 
active antiretroviral agent to minimise the potential for virologic failure and the development of 
resistance (see section 5.1). 
 
Co-administration of other medicinal products 
Elvitegravir is primarily metabolised by CYP3A.  Co-administration of Vitekta with strong CYP3A 
inducers (including St. John’s wort [Hypericum perforatum], rifampicin, carbamazepine, 
phenobarbital and phenytoin) is contraindicated (see sections 4.3 and 4.5).  Co-administration of 
Vitekta with moderate CYP3A inducers (including, but not limited to, efavirenz and bosentan) is not 
recommended (see section 4.5). 
 
Due to the need for co-administration of Vitekta with a ritonavir-boosted protease inhibitor, 
prescribers should consult the Summary of Product Characteristics of the co-administered protease 
inhibitor and ritonavir for a description of contraindicated medicinal products and other significant 
drug-drug interactions that may cause potentially life-threatening adverse reactions or loss of 
therapeutic effect and possible development of resistance. 
 
Atazanavir/ritonavir and lopinavir/ritonavir have been shown to significantly increase the plasma 
concentrations of elvitegravir (see section 4.5).  When used in combination with atazanavir/ritonavir 
and lopinavir/ritonavir, the dose of Vitekta should be decreased from 150 mg once daily to 85 mg once 
daily (see section 4.2).  Please refer to the Summary of Product Characteristics for Vitekta 85 mg 
tablets. 
 
Co-administration of Vitekta and related active substances: Vitekta must be used in combination with 
a ritonavir-boosted protease inhibitor.  Vitekta should not be used with a protease inhibitor boosted by 
another agent as dosing recommendations for such combinations have not been established.  Boosting 
elvitegravir with an agent other than ritonavir may result in suboptimal plasma concentrations of 
elvitegravir and/or the protease inhibitor leading to loss of therapeutic effect and possible development 
of resistance. 
 
Vitekta should not be used in combination with products containing elvitegravir or pharmacokinetic 
boosting agents other than ritonavir. 
 
Contraception requirements 
Female patients of childbearing potential should use either a hormonal contraceptive containing at 
least 30 µg ethinylestradiol and containing norgestimate as the progestagen or should use an 
alternative reliable method of contraception (see sections 4.5 and 4.6).  Co-administration of 
elvitegravir with oral contraceptives containing progestagens other than norgestimate have not been 
studied and, therefore, should be avoided. 
 

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Patients using oestrogens as hormone replacement therapy should be clinically monitored for signs of 
oestrogen deficiency (see section 4.5). 
 
Opportunistic infections 
Patients receiving Vitekta or any other antiretroviral therapy may continue to develop opportunistic 
infections and other complications of HIV infection, and therefore should remain under close clinical 
observation by physicians experienced in the treatment of patients with HIV associated diseases. 
 
Patients with HIV and hepatitis B or C virus co-infection 
Patients with chronic hepatitis B or C treated with antiretroviral therapy are at an increased risk for 
severe and potentially fatal hepatic adverse reactions. 
 
Physicians should refer to current HIV treatment guidelines for the optimal management of 
HIV infection in patients co-infected with hepatitis B virus (HBV). 
 
Liver disease 
Elvitegravir has not been studied in patients with severe hepatic impairment (Child-Pugh Class C).  No 
dose adjustment of Vitekta is required in patients with mild (Child-Pugh Class A) or moderate hepatic 
impairment (Child-Pugh Class B) (see sections 4.2 and 5.2). 
 
Patients with pre-existing liver dysfunction, including chronic active hepatitis, have an increased 
frequency of liver function abnormalities during combination antiretroviral therapy (CART) and 
should be monitored according to standard practice.  If there is evidence of worsening liver disease in 
such patients, interruption or discontinuation of treatment must be considered. 
 
Weight and metabolic parameters 
An increase in weight and in levels of blood lipids and glucose may occur during antiretroviral 
therapy.  Such changes may in part be linked to disease control and life style.  For lipids, there is in 
some cases evidence for a treatment effect, while for weight gain there is no strong evidence relating 
this to any particular treatment.  For monitoring of blood lipids and glucose reference is made to 
established HIV treatment guidelines.  Lipid disorders should be managed as clinically appropriate. 
 
Immune Reactivation Syndrome 
In HIV infected patients with severe immune deficiency at the time of institution of CART, an 
inflammatory reaction to asymptomatic or residual opportunistic pathogens may arise and cause 
serious clinical conditions, or aggravation of symptoms.  Typically, such reactions have been observed 
within the first few weeks or months of initiation of CART.  Relevant examples are cytomegalovirus 
retinitis, generalised and/or focal mycobacterial infections, and Pneumocystis jirovecii pneumonia.  
Any inflammatory symptoms should be evaluated and treatment instituted when necessary. 
 
Autoimmune disorders (such as Graves’ disease) have also been reported to occur in the setting of 
immune reactivation; however, the reported time to onset is more variable and these events can occur 
many months after initiation of treatment. 
 
Osteonecrosis 
Although the aetiology is considered to be multifactorial (including corticosteroid use, alcohol 
consumption, severe immunosuppression, higher body mass index), cases of osteonecrosis have been 
reported particularly in patients with advanced HIV disease and/or long-term exposure to CART.  
Patients should be advised to seek medical advice if they experience joint aches and pain, joint 
stiffness or difficulty in movement. 
 
Excipients 
Vitekta contains lactose.  Consequently, patients with rare hereditary problems of galactose 
intolerance, the Lapp lactase deficiency, or glucose-galactose malabsorption should not take this 
medicinal product. 
 

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4.5 Interaction with other medicinal products and other forms of interaction 
 
Interaction studies have only been performed in adults. 
 
Interactions with CYP3A inducers 
Elvitegravir is primarily metabolised by CYP3A (see section 5.2).  Medicinal products that are strong 
(causing a > 5-fold increase in substrate clearance) or moderate (causing a 2-5 fold increase in 
substrate clearance) inducers of CYP3A are expected to decrease plasma concentrations of 
elvitegravir. 
 
Concomitant use contraindicated 
Co-administration of Vitekta with medicinal products that are strong inducers of CYP3A is 
contraindicated as the expected decrease in plasma concentrations of elvitegravir can lead to loss of 
therapeutic effect and possible development of resistance to elvitegravir (see section 4.3). 
 
Concomitant use not recommended 
Co-administration of Vitekta with medicinal products that are moderate inducers of CYP3A 
(including, but not limited to, efavirenz and bosentan) is not recommended as the expected decrease in 
plasma concentrations of elvitegravir can lead to loss of therapeutic effect and possible development 
of resistance to elvitegravir (see section 4.4). 
 
Interactions requiring dose adjustment of Vitekta 
Elvitegravir undergoes oxidative metabolism by CYP3A (major route), and glucuronidation by 
UGT1A1/3 enzymes (minor route).  Co-administration of Vitekta with medicinal products that are 
potent inhibitors of UGT1A1/3 may result in increased elvitegravir plasma concentrations and dose 
modifications may be required.  For example, atazanavir/ritonavir and lopinavir/ritonavir (potent 
UGT1A1/3 inhibitors) have been shown to significantly increase the plasma concentrations of 
elvitegravir (see Table 2).  Accordingly, when used in combination with atazanavir/ritonavir and 
lopinavir/ritonavir, the dose of Vitekta should be decreased from 150 mg once daily to 85 mg once 
daily (see sections 4.2 and 4.4).  Please refer to the Summary of Product Characteristics for Vitekta 
85 mg tablets. 
 
Other interactions 
Elvitegravir is a modest inducer and may have the potential to induce CYP2C9 and/or inducible UGT 
enzymes.  As such, elvitegravir may decrease the plasma concentration of substrates of CYP2C9 (such 
as warfarin) or UGT (such as ethinyl estradiol).  In addition, in vitro studies have shown that 
elvitegravir is a weak to modest inducer of CYP1A2, CYP2C19 and CYP3A enzymes.  Elvitegravir 
would also have potential to be a weak to modest inducer of CYP2B6 and CYP2C8 enzymes, as these 
enzymes are regulated in a similar manner to CYP2C9 and CYP3A.  However, clinical data have 
shown there are no clinically relevant changes in the exposure of methadone (which is primarily 
metabolised by CYP2B6 and CYP2C19) following co-administration with boosted elvitegravir versus 
administration of methadone alone (see Table 2). 
 
Elvitegravir is a substrate for OATP1B1 and OATP1B3, and an inhibitor of OATP1B3 in vitro.  The 
in vivo relevance of these interactions is not clear. 
 
Interactions between elvitegravir and potential co-administered medicinal products are listed in 
Table 2 below (increase is indicated as “↑”, decrease as “↓”, no change as “↔”).  These interactions 
are based on either drug interaction studies or predicted interactions due to the expected magnitude of 
interaction and potential for serious adverse events or loss of therapeutic effect. 
 
Where interactions were studied, the effect on Vitekta was determined by comparing the 
pharmacokinetics of boosted elvitegravir (using either ritonavir or cobicistat as a pharmacokinetic 
enhancer) in the absence and presence of the co-administered medicinal product.  No interactions were 
studied using unboosted elvitegravir.  Except where indicated in Table 2, the dose of boosted 
elvitegravir or co-administered medicinal product was the same when administered alone or in 

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combination.  The pharmacokinetic parameters of the protease inhibitors presented in Table 2 were 
assessed in the presence of ritonavir. 
 
Although there may be no actual or predicted interactions between a medicinal product and 
elvitegravir, there may be interactions between a medicinal product and ritonavir and/or the protease 
inhibitor co-administered with elvitegravir.  The prescriber should always refer to the Summary of 
Product Characteristics for ritonavir, or the protease inhibitor. 
 
Table 2: Interactions between elvitegravir and other medicinal products 
 

Medicinal product by 
therapeutic areas 

Effects on drug levels 
Mean percent change in AUC, 

Cmax, Cmin 

Recommendation concerning 
co-administration with 

ritonavir-boosted elvitegravir 
ANTIRETROVIRALS 
HIV protease inhibitors 
Atazanavir (300 mg once daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (100 mg once daily) 

Atazanavir/Ritonavir has been 
shown to significantly increase 
the plasma concentrations of 
elvitegravir. 
 
Elvitegravir: 
AUC: ↑ 100% 
Cmax: ↑ 85% 
Cmin: ↑ 188% 
 
Atazanavir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↓ 35% 

When used in combination with 
atazanavir, the dose of Vitekta 
should be 85 mg once daily.  
When used in combination with 
Vitekta, the recommended dose of 
atazanavir is 300 mg with 
ritonavir 100 mg once daily. 
 
There are no data available to 
make dosing recommendations for 
co-administration with other doses 
of atazanavir (see section 4.2). 

Atazanavir (300 mg once daily) 
Elvitegravir (85 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔* 
Cmax: ↔* 
Cmin: ↑ 38%* 
 
Atazanavir: 
AUC: ↔** 
Cmax: ↔** 
Cmin: ↔** 
 
*when compared to 
elvitegravir/ritonavir 
150/100 mg once daily. 
 
**when compared to 
atazanavir/ritonavir 300/100 mg 
once daily. 

Darunavir (600 mg twice daily) 
Elvitegravir (125 mg once daily) 
Ritonavir (100 mg twice daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Darunavir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↓ 17% 

When used in combination with 
darunavir, the dose of Vitekta 
should be 150 mg once daily. 
 
There are no data available to 
make dosing recommendations for 
co-administration with other doses 
of darunavir (see section 4.2). M

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Fosamprenavir (700 mg twice 
daily) 
Elvitegravir (125 mg once daily) 
Ritonavir (100 mg twice daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Fosamprenavir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

When used in combination with 
fosamprenavir, the dose of Vitekta 
should be 150 mg once daily. 
 
There are no data available to 
make dosing recommendations for 
co-administration with other doses 
of fosamprenavir (see section 4.2). 

Lopinavir/Ritonavir (400/100 mg 
twice daily) 
Elvitegravir (125 mg once daily) 

Lopinavir/Ritonavir has been 
shown to significantly increase 
the plasma concentrations of 
elvitegravir. 
 
Elvitegravir: 
AUC: ↑ 75% 
Cmax: ↑ 52% 
Cmin: ↑ 138% 
 
Lopinavir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↓ 8% 

When used in combination with 
lopinavir/ritonavir, the dose of 
Vitekta should be 85 mg once 
daily. 
 
There are no data available to 
make dosing recommendations for 
co-administration with other doses 
of lopinavir/ritonavir (see 
section 4.2). 

Tipranavir (500 mg twice daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (200 mg twice daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Tipranavir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↓ 11% 

Due to insufficient clinical data, 
the combination of elvitegravir 
with tipranavir is not 
recommended (see section 4.2). 

NRTIs 
Didanosine (400 mg once daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Didanosine: 
AUC: ↓ 14% 
Cmax: ↓ 16% 

As didanosine is administered on 
an empty stomach, didanosine 
should be administered at least 
one hour before or two hours after 
Vitekta (which is administered 
with food).  Clinical monitoring is 
recommended. 

Zidovudine (300 mg twice daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Zidovudine: 
AUC: ↔ 
Cmax: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with zidovudine. 

Stavudine (40 mg once daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Stavudine: 
AUC: ↔ 
Cmax: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with stavudine. Me

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Abacavir (600 mg once daily) 
Elvitegravir (200 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Abacavir: 
AUC: ↔ 
Cmax: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with abacavir. 

Tenofovir disoproxil fumarate 
(300 mg once daily) 
Emtricitabine (200 mg once daily) 
Elvitegravir (50 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Tenofovir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Emtricitabine: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with tenofovir disoproxil fumarate 
or with emtricitabine. 

NNRTIs 
Efavirenz Interaction not studied with 

elvitegravir. 
 
Co-administration of efavirenz 
and elvitegravir is expected to 
decrease elvitegravir plasma 
concentrations which may result 
in loss of therapeutic effect and 
possible development of 
resistance. 

Co-administration is not 
recommended (see section 4.4). 

Etravirine (200 mg twice daily) 
Elvitegravir (150 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Etravirine: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with etravirine. 

Nevirapine Interaction not studied with 
elvitegravir. 
 
Co-administration of nevirapine 
and elvitegravir is expected to 
decrease elvitegravir plasma 
concentrations which may result 
in loss of therapeutic effect and 
possible development of 
resistance. 

Co-administration is not 
recommended (see section 4.4). 

Rilpivirine Interaction not studied with 
elvitegravir. 

Co-administration of elvitegravir 
and rilpivirine is not expected to 
change elvitegravir plasma 
concentrations, therefore no dose 
adjustment of Vitekta is required. 

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CCR5 antagonists 
Maraviroc (150 mg twice daily) 
Elvitegravir (150 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Maraviroc:§ 
AUC: ↑ 186% 
Cmax: ↑ 115% 
Cmin: ↑ 323% 

No dose adjustment is required 
when Vitekta is co-administered 
with maraviroc. 
 
§Due to inhibition of CYP3A by 
ritonavir, maraviroc exposure is 
significantly increased. 

ANTACIDS 
Magnesium/aluminum-containing 
antacid suspension (20 mL single 
dose) 
Elvitegravir (50 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir (antacid suspension 
given ± 4 hours from 
elvitegravir administration): 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Elvitegravir (simultaneous 
antacid administration): 
AUC: ↓ 45% 
Cmax: ↓ 47% 
Cmin: ↓ 41% 

Elvitegravir plasma concentrations 
are lower with antacids due to 
local complexation in the 
gastrointestinal tract and not to 
changes in gastric pH.  It is 
recommended to separate Vitekta 
and antacid administration by at 
least 4 hours. 

FOOD SUPPLEMENTS 
Multivitamin supplements Interaction not studied with 

elvitegravir. 
As the effect of cationic 
complexation of elvitegravir 
cannot be excluded when 
co-administered with multivitamin 
supplements, it is recommended to 
separate Vitekta and multivitamin 
supplements dosing by at least 
4 hours. 

NARCOTIC ANALGESICS 
Methadone (80-120 mg once daily) 
Elvitegravir (150 mg once daily) 
Cobicistat (150 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Methadone: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with methadone. 

Buprenorphine/Naloxone (16/4 mg 
to 24/6 mg daily) 
Elvitegravir (150 mg once daily) 
Cobicistat (150 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Buprenorphine: 
AUC: ↑ 35% 
Cmax: ↑ 12% 
Cmin: ↑ 66% 
 
Naloxone: 
AUC: ↓ 28% 
Cmax: ↓ 28% 

No dose adjustment is required 
when Vitekta is co-administered 
with buprenorphine/naloxone. 

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ANTI-INFECTIVES 
Antifungals 
Ketoconazole (200 mg twice daily) 
Elvitegravir (150 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↑ 48% 
Cmax: ↔ 
Cmin: ↑ 67% 
 
↑ Ketoconazole§ 

No dose adjustment is required 
when Vitekta is co-administered 
with ketoconazole. 
 
§Due to inhibition of CYP3A by 
ritonavir, ketoconazole exposure is 
increased. 

Antimycobacterials 
Rifabutin (150 mg once every 
other day) 
Elvitegravir (300 mg once daily) 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔* 
Cmax: ↔* 
Cmin: ↔* 
 
Rifabutin: 
AUC: ↔** 
Cmax: ↔** 
Cmin: ↔** 

Co-administration of Vitekta and 
rifabutin is not recommended.  If 
the combination is needed, the 
recommended dose of rifabutin is 
150 mg 3 times per week on set 
days (for example Monday-
Wednesday-Friday). 
 
No dose adjustment of Vitekta is 
required when co-administered 
with reduced dose of rifabutin. 
 
Further dose reduction of rifabutin 
has not been studied.  It should be 
kept in mind that a twice weekly 
dose of 150 mg may not provide 
an optimal exposure to rifabutin 
thus leading to a risk of rifamycin 
resistance and a treatment failure. 
 
§Due to inhibition of CYP3A by 
ritonavir, 25-O-desacetyl-rifabutin 
exposure is increased. 

 25-O-desacetyl-rifabutin:§ 
AUC: ↑ 851%** 
Cmax: ↑ 440%** 
Cmin: ↑ 1,836%** 
 
*when compared to 
elvitegravir/ritonavir 
300/100 mg once daily. 
 
**when compared to rifabutin 
300 mg once daily. 
 
Total antimycobacterial activity 
was increased by 50%. 

ANTICOAGULANTS 
Warfarin Interaction not studied with 

elvitegravir. 
 
Concentrations of warfarin may 
be affected upon 
co-administration with 
elvitegravir. 

It is recommended that the 
international normalised ratio 
(INR) be monitored upon 
co-administration of Vitekta.  INR 
should continue to be monitored 
during the first weeks following 
cessation of treatment with 
Vitekta. 

H2-RECEPTOR ANTAGONISTS 
Famotidine (40 mg once daily) 
Elvitegravir (150 mg once daily) 
Cobicistat (150 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with famotidine. 

HMG-CoA REDUCTASE INHIBITORS 
Rosuvastatin (10 mg single dose) 
Elvitegravir (150 mg once daily) 
Cobicistat (150 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 
 
Rosuvastatin: 
AUC: ↑ 38% 
Cmax: ↑ 89% 
Cmin: ↑ 43% 

No dose adjustment is required 
when Vitekta is co-administered 
with rosuvastatin. 

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Atorvastatin 
Fluvastatin 
Pitavastatin 
Pravastatin 

Interaction not studied with 
elvitegravir. 
 
Plasma concentrations of OATP 
substrates are not expected to 
change upon co-administration 
of elvitegravir. 
 
Plasma concentrations of 
elvitegravir are not expected to 
change upon co-administration 
of OATP substrates/inhibitors. 

No dose adjustment is required 
when Vitekta is co-administered 
with atorvastatin, fluvastatin, 
pitavastatin or pravastatin. 

ORAL CONTRACEPTIVES 
Norgestimate (0.180/0.215 mg 
once daily) 
Ethinylestradiol (0.025 mg once 
daily) 
Elvitegravir (150 mg once daily) 
Cobicistat (150 mg once daily)1 
 

Norgestimate: 
AUC: ↑ 126% 
Cmax: ↑ 108% 
Cmin: ↑ 167% 
 
Ethinylestradiol: 
AUC: ↓ 25% 
Cmax: ↔ 
Cmin: ↓ 44% 
 
Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

Caution should be exercised when 
co-administering Vitekta and a 
hormonal contraceptive.  The 
hormonal contraceptive should 
contain at least 30 µg 
ethinylestradiol and contain 
norgestimate as the progestagen or 
patients should use an alternative 
reliable method of contraception 
(see sections 4.4 and 4.6). 
 
The long-term effects of 
substantial increases in 
progesterone exposure are 
unknown.  Co-administration of 
elvitegravir with oral 
contraceptives containing 
progestagens other than 
norgestimate has not been studied 
and therefore should be avoided. 

PROTON PUMP INHIBITORS 
Omeprazole (40 mg once daily) 
Elvitegravir (50 mg once daily 
Ritonavir (100 mg once daily) 

Elvitegravir: 
AUC: ↔ 
Cmax: ↔ 
Cmin: ↔ 

No dose adjustment is required 
when Vitekta is co-administered 
with omeprazole. 

1 This study was conducted using the fixed-dose combination tablet elvitegravir/cobicistat/emtricitabine/tenofovir 
disoproxil. 

 
4.6 Fertility, pregnancy and lactation 
 
Women of childbearing potential / contraception in males and females 
The use of Vitekta must be accompanied by the use of effective contraception (see sections 4.4 
and 4.5). 
 
Pregnancy 
There are no or limited clinical data with elvitegravir in pregnant women. 
 
Animal studies do not indicate direct or indirect harmful effects of elvitegravir with respect to 
reproductive toxicity.  However, the maximum exposures evaluated in the rabbit were not in excess of 
those achieved therapeutically (see section 5.3). 
 
Vitekta should not be used during pregnancy unless the clinical condition of the woman requires 
treatment with elvitegravir. 
 
Breast-feeding 
It is unknown whether elvitegravir/metabolites are excreted in human milk.  Available 
pharmacodynamic/toxicological data in rats have shown excretion of elvitegravir in milk.  A risk to 

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the newborns/infants cannot be excluded.  Therefore, Vitekta should not be used during breast-
feeding. 
 
In order to avoid transmission of HIV to the infant it is recommended that HIV infected women do not 
breast-feed their infants under any circumstances. 
 
Fertility 
No human data on the effect of elvitegravir on fertility are available.  Animal studies do not indicate 
harmful effects of elvitegravir on fertility. 
 
4.7 Effects on ability to drive and use machines 
 
No studies on the effects of elvitegravir on the ability to drive and use machines have been performed. 
 
4.8 Undesirable effects 
 
Summary of the safety profile 
Assessment of adverse reactions is based on data from a controlled clinical study (GS-US-183-0145) 
in which 712 HIV-1 infected, antiretroviral treatment-experienced adults received elvitegravir 
(n = 354) or raltegravir (n = 358) each administered with a background regimen consisting of a fully 
active ritonavir-boosted protease inhibitor and other antiretroviral agents.  Of these 712 patients, 543 
(269 elvitegravir and 274 raltegravir) and 439 (224 elvitegravir and 215 raltegravir) received at least 
48 and 96 weeks of treatment, respectively. 
 
The most frequently reported adverse reactions to elvitegravir were diarrhoea (7.1%) and nausea 
(4.0%) (see Table 3). 
 
Tabulated summary of adverse reactions 
Adverse reactions to elvitegravir from clinical study experience are listed in Table 3 below, by body 
system organ class and frequency.  Within each frequency grouping, undesirable effects are presented 
in order of decreasing seriousness.  Frequencies are defined as common (≥ 1/100 to < 1/10) or 
uncommon (≥ 1/1,000 to < 1/100). 
 
Table 3: Tabulated summary of adverse reactions to elvitegravir based on experience for 
96 weeks from clinical study GS-US-183-0145 
 
Frequency Adverse reaction 
Psychiatric disorders: 

Uncommon suicidal ideation and suicide attempt (in patients with a pre-existing history of depression or psychiatric illness), depression, insomnia 
Nervous system disorders: 
Common headache 
Uncommon dizziness, paraesthesia, somnolence, dysgeusia 
Gastrointestinal disorders: 
Common abdominal pain, diarrhoea, vomiting, nausea 
Uncommon dyspepsia, abdominal distension, flatulence 
Skin and subcutaneous tissue disorders: 
Common rash 
General disorders and administration site conditions: 
Common fatigue 
 
Description of selected adverse reactions 
 
Metabolic parameters 
Weight and levels of blood lipids and glucose may increase during antiretroviral therapy (see 
section 4.4). 
 

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Immune Reactivation Syndrome 
In HIV infected patients with severe immune deficiency at the time of initiation of CART, an 
inflammatory reaction to asymptomatic or residual opportunistic infections may arise.  Autoimmune 
disorders (such as Graves’ disease) have also been reported; however, the reported time to onset is 
more variable and these events can occur many months after initiation of treatment (see section 4.4). 
 
Osteonecrosis 
Cases of osteonecrosis have been reported, particularly in patients with generally acknowledged risk 
factors, advanced HIV disease or long-term exposure to CART.  The frequency of this is unknown 
(see section 4.4). 
 
Diarrhoea 
In study GS-US-183-0145, diarrhoea was reported as an adverse reaction in 7.1% of subjects in the 
elvitegravir group and in 5.3% of subjects in the raltegravir group.  In these subjects, diarrhoea was 
mild to moderate in severity and did not result in discontinuation of study drug. 
 
Paediatric population 
No data are available for children below 18 years of age.  Vitekta is not recommended in this 
population (see section 4.2). 
 
Reporting of suspected adverse reactions 
Reporting suspected adverse reactions after authorisation of the medicinal product is important.  It 
allows continued monitoring of the benefit/risk balance of the medicinal product.  Healthcare 
professionals are asked to report any suspected adverse reactions via the national reporting system 
listed in Appendix V. 
 
4.9 Overdose 
 
If overdose occurs the patient must be monitored for evidence of toxicity.  Treatment of overdose with 
elvitegravir consists of general supportive measures including monitoring of vital signs as well as 
observation of the clinical status of the patient. 
 
There is no specific antidote for overdose with elvitegravir.  As elvitegravir is highly bound to plasma 
proteins, it is unlikely that it will be significantly removed by haemodialysis or peritoneal dialysis. 
 
 
5. PHARMACOLOGICAL PROPERTIES 
 
5.1 Pharmacodynamic properties 
 
Pharmacotherapeutic group: Antivirals for systemic use, other antivirals, ATC code: J05AX11. 
 
Mechanism of action and pharmacodynamic effects 
Elvitegravir is an HIV-1 integrase strand transfer inhibitor (INSTI).  Integrase is an HIV-1 encoded 
enzyme that is required for viral replication.  Inhibition of integrase prevents the integration of 
HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation 
of the viral infection.  Elvitegravir does not inhibit human topoisomerases I or II. 
 
Antiviral activity in vitro 
The antiviral activity of elvitegravir against laboratory and clinical isolates of HIV-1 was assessed in 
lymphoblastoid cells, monocyte/macrophage cells, and peripheral blood lymphocytes and the 50% 
effective concentration (EC50) values were in the range of 0.02 to 1.7 nM.  Elvitegravir displayed 
antiviral activity in cell culture against HIV-1 clades A, B, C, D, E, F, G, and O (EC50 values ranged 
from 0.1 to 1.3 nM) and activity against HIV-2 (EC50 of 0.53 nM).  The in vitro antiviral activity of 
elvitegravir when combined with antiretroviral drugs from the nucleos(t)ide reverse transcriptase 
inhibitor (NRTI), non-nucleoside reverse transcriptase inhibitor (NNRTI), protease inhibitor (PI), 

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35 

integrase strand transfer inhibitor, fusion inhibitor, or CCR5 co-receptor antagonist classes showed no 
antagonism. 
 
Elvitegravir did not show inhibition of replication of HBV or HCV in vitro. 
 
Resistance 
In cell culture 
HIV-1 isolates with reduced susceptibility to elvitegravir have been selected in cell culture.  
Phenotypic resistance to elvitegravir was most commonly associated with the primary integrase 
substitutions T66I, E92Q and Q148R.  Additional integrase substitutions observed in cell culture 
selection included H51Y, F121Y, S147G, S153Y, E157Q, and R263K. 
 
Cross resistance 
Elvitegravir-resistant viruses show varying degrees of cross-resistance to the integrase strand transfer 
inhibitor raltegravir depending on the type and number of substitutions.  Viruses expressing the 
T66I/A substitutions maintain susceptibility to raltegravir, while most other patterns of 
elvitegravir-associated substitutions are associated with reduced susceptibility to raltegravir.  With the 
exception of Y143C/R/H, HIV-1 with the primary raltegravir-associated substitutions T66K, 
Q148H/K/R, or N155H in integrase is associated with reduced susceptibility to elvitegravir. 
 
In treatment-experienced patients 
In an analysis of HIV-1 isolates from treatment-failure subjects in study GS-US-183-0145 through 
week 96, the development of one or more primary elvitegravir resistance-associated substitutions was 
observed in 23 of the 86 subjects with evaluable genotypic data from paired baseline and elvitegravir 
treatment-failure isolates (23/351 elvitegravir-treated subjects, 6.6%).  Similar rates of raltegravir 
resistance development occurred in the HIV-1 from subjects treated with raltegravir (26/351 
raltegravir-treated subjects, 7.4%).  The most common substitutions that emerged in HIV-1 isolates 
from elvitegravir-treated subjects were T66I/A (n = 8), E92Q/G (n = 7), T97A (n = 4), S147G (n = 4), 
Q148R (n = 4), and N155H (n = 5) in integrase.  In phenotypic analyses of HIV-1 isolates with 
resistance substitutions from elvitegravir-treated subjects, 14/20 (70%) had reduced susceptibility to 
elvitegravir and 12/20 (60%) had reduced susceptibility to raltegravir. 
 
Clinical experience 
In treatment-experienced HIV-1 infected patients 
The efficacy of elvitegravir is primarily based on the analyses through 96 weeks from one randomised, 
double-blind, active-controlled study, study GS-US-183-0145, in treatment-experienced, 
HIV-1 infected patients (n = 702). 
 
In study GS-US-183-0145, patients were randomised in a 1:1 ratio to receive either elvitegravir 
(150 mg or 85 mg) once daily or raltegravir 400 mg twice daily, each administered with a background 
regimen (BR) containing a fully-active ritonavir-boosted protease inhibitor (either atazanavir, 
darunavir, fosamprenavir, lopinavir or tipranavir) and a second agent.  The BR was selected by the 
investigator based on genotypic/phenotypic resistance testing and prior antiretroviral treatment history.  
Randomisation was stratified by screening HIV-1 RNA level (≤ 100,000 copies/mL or 
> 100,000 copies/mL) and the class of the second agent (NRTI or other classes).  Virologic response 
rate was evaluated in both treatment arms.  Virologic response was defined as achieving an 
undetectable viral load (HIV-1 RNA < 50 copies/mL). 
 
Baseline characteristics and treatment outcomes through 96 weeks for study GS-US-183-0145 are 
presented in Tables 4 and 5 respectively. 
 

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Table 4: Demographic and baseline disease characteristics of antiretroviral treatment-
experienced HIV-1 infected adult subjects in study GS-US-183-0145 
 
 
 

Elvitegravir + background 
regimen 
n = 351 

Raltegravir + background 
regimen 
n = 351 

Demographic characteristics 
Median age, years (min-max) 44 

(20-78) 
45 

(19-74) 
Sex   
 Male 83.2% 80.9% 
 Female 16.8% 19.1% 
Ethnicity   
 White 60.1% 64.4% 
 Black/African American 35.6% 32.2% 
 Asian 2.6% 1.4% 
 Other 1.7% 2.0% 
Baseline disease characteristics 
Median baseline plasma 
HIV-1 RNA (range) 
log10 copies/mL 

4.35 
(1.69-6.63) 

4.42 
(1.69-6.10) 

Percentage of subjects with 
viral load > 100,000 copies/mL 

25.6 25.6 

Median baseline CD4+ cell 
count (range), cells/mm3 

227.0 
(2.0-1,374.0) 

215.0 
(1.0-1,497.0) 

Percentage of subjects with 
CD4+ cell counts 
≤ 200 cells/mm3 

44.4 
 

44.9 

Baseline genotypic sensitivity 
scorea 

0 
1 
2 
3 

 
 

1% 
14% 
81% 
3% 

 
 

< 1% 
15% 
83% 
2% 

a Genotypic sensitivity scores are calculated by summing up drug susceptibility values (1 = sensitive; 0 = reduced 
susceptibility) on all drugs in the baseline background regimen. 

 
Table 5: Virologic outcome of randomised treatment of study GS-US-183-0145 at week 48 and 
week 96 (snapshot analysis)a 
 
 Week 48 Week 96 
 Elvitegravir 

+ background 
regimen 
n = 351 

Raltegravir 
+ background 

regimen 
n = 351 

Elvitegravir 
+ background 

regimen 
n = 351 

Raltegravir 
+ background 

regimen 
n = 351 

Virologic success 
HIV-1 RNA 
< 50 copies/mL 

60% 58% 52% 53% 

Treatment difference 2.2% (95% CI = -5.0%, 9.3%) -0.5% (95% CI = -7.9%, 6.8%) 
Virologic failureb 33% 32% 36% 31% 
No virologic data at 
week 48 or week 96 
window 

7% 11% 12% 16% 

Discontinued study drug 
due to AE or deathc 

2% 5% 3% 7% 

Discontinued study drug 4% 5% 8% 9% 

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 Week 48 Week 96 
 Elvitegravir 

+ background 
regimen 
n = 351 

Raltegravir 
+ background 

regimen 
n = 351 

Elvitegravir 
+ background 

regimen 
n = 351 

Raltegravir 
+ background 

regimen 
n = 351 

due to other reasons and 
last available 
HIV-1 RNA 
< 50 copies/mLd 
Missing data during 
window but on study 
drug 

1% 1% 1% 1% 

a Week 48 window is between day 309 and 364 (inclusive), week 96 window is between day 645 and 700 (inclusive). 
b Includes subjects who had ≥ 50 copies/mL in the week 48 or week 96 window, subjects who discontinued early due to 

lack or loss of efficacy, subjects who had a viral load ≥ 50 copies/mL at time of change in background regimen, subjects 
who discontinued for reasons other than an adverse event (AE), death or lack or loss of efficacy and at the time of 
discontinuation had a viral load of ≥ 50 copies/mL. 

c Includes patients who discontinued due to an AE or death at any time point from day 1 through the time window if this 
resulted in no virologic data on treatment during the specified window. 

d Includes subjects who discontinued for reasons other than an AE, death or lack or loss of efficacy, e.g., withdrew consent, 
loss to follow-up, etc. 

 
Elvitegravir was non-inferior in achieving HIV-1 RNA < 50 copies/mL when compared to raltegravir. 
 
Among subjects with a genotypic sensitivity score of ≤ 1, 76% and 69% had HIV-1 RNA 
< 50 copies/mL at week 48 in the elvitegravir and raltegravir treatment arms, respectively.  Among 
subjects with a genotypic sensitivity score > 1, 57% and 56% had HIV-1 RNA < 50 copies/mL at 
week 48 in the elvitegravir and raltegravir treatment arms, respectively. 
 
In study GS-US-183-0145, the mean increase from baseline in CD4+ cell count at week 96 was 
205 cells/mm3 in the elvitegravir-treated patients and 198 cells/mm3 in the raltegravir-treated patients. 
 
In study GS-US-183-0145, subgroup analyses by co-administered protease inhibitor showed similar 
rates of virologic success for elvitegravir and raltegravir within each protease inhibitor subgroup at 
weeks 48 and 96 (HIV-1 RNA < 50 copies/mL) (Table 6). 
 
Table 6: Virologic success by co-administered protease inhibitor in study GS-US-183-0145 at 
week 48 and week 96 (snapshot analysis) 
 
  Elvitegravir versus 

raltegravir 
HIV-1 RNA 
< 50 copies/mL, n/N (%) 

Elvitegravir 
(N = 351) 

Raltegravir 
(N = 351) 

Difference in percentages 
(95% CI)a 

Virologic success at 
week 48 

   

Darunavir/ritonavir 126/202 (62.4%) 122/207 (58.9%) 3.4% (-6.0% to 12.9%) 
Lopinavir/ritonavir 39/68 (57.4%) 37/68 (54.4%) 2.9% (-13.7% to 19.6%) 
Atazanavir/ritonavir 34/61 (55.7%) 28/51 (54.9%) 0.8% (-17.7% to 19.3%) 
Fosamprenavir/ritonavir 8/14 (57.1%) 10/18 (55.6%) 1.6% (-33.0% to 36.2%) 
Tipranavir/ritonavir 3/6 (50.0%) 5/7 (71.4%) -21.4% (-73.6% to 30.7%) 

Virologic success at 
week 96 

   

Darunavir/ritonavir 105/202 (52.0%) 112/207 (54.1%) -2.1% (-11.8% to 7.5%) 
Lopinavir/ritonavir 36/68 (52.9%) 37/68 (54.4%) -1.5% (-18.2% to 15.3%) 
Atazanavir/ritonavir 33/61 (54.1%) 23/51 (45.1%) 9.0% (-9.5% to 27.5%) 
Fosamprenavir/ritonavir 7/14 (50.0%) 11/18 (61.1%) -11.1% (-45.7% to 23.4%) 
Tipranavir/ritonavir 3/6 (50.0%) 3/7 (42.9%) 7.1% (-47.1% to 61.4%) 

a The difference in proportions and its 95% CIs between randomised treatment groups is based on normal approximation. 

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Although limited by the small number of female subjects in study GS-US-183-0145, subgroup 
analysis by gender showed that the rates of virologic success in female subjects at weeks 48 and 96 
(HIV-1 RNA < 50 copies/mL) were numerically lower in the elvitegravir treatment arm than in the 
raltegravir treatment arm.  Virologic success rates at week 48 for elvitegravir and raltegravir were 
47.5% (28/59) and 62.7% (42/67) (difference: -12.3% [95% CI: -30.1% to 5.5%]), respectively, for 
female subjects, and 62.3% (182/292) and 56.3% (160/284) (difference: 5.3% [95% CI: -2.5% to 
13.2%]), respectively, for male subjects.  Virologic success rates at week 96 for elvitegravir and 
raltegravir were 39.0% (23/59) and 52.2% (35/67) (difference: -8.4% [95% CI: -26.1% to 9.2%]), 
respectively, for female subjects, and 55.1% (161/292) and 53.2% (151/284) (difference: 1.5% 
[95% CI: -6.5% to 9.6%]), respectively, for male subjects. 
 
Paediatric population 
The European Medicines Agency has deferred the obligation to submit the results of studies with 
elvitegravir in one or more subsets of the paediatric population in the treatment of HIV-1 infection 
(see section 4.2 for information on paediatric use). 
 
5.2 Pharmacokinetic properties 
 
Absorption 
Following oral administration of ritonavir-boosted elvitegravir with food in HIV-1 infected subjects, 
elvitegravir peak plasma concentrations were observed 4 hours post-dose.  The steady-state mean Cmax, 
AUCtau, and Ctrough (mean ± SD) following multiple doses of elvitegravir plus a ritonavir-boosted 
protease inhibitor (150 mg elvitegravir with darunavir or fosamprenavir; 85 mg elvitegravir with 
atazanavir or lopinavir) in HIV-1 infected subjects were 1.4 ± 0.39 μg/mL, 18 ± 6.8 μg•h/mL, and 
0.38 ± 0.22 μg/mL for elvitegravir, respectively.  The absolute oral bioavailability has not been 
determined. 
 
Relative to fasting conditions, the administration of boosted elvitegravir as the fixed-dose combination 
150 mg elvitegravir/150 mg cobicistat/200 mg emtricitabine/245 mg tenofovir disoproxil with a light 
meal (approximately 373 kcal, 20% fat) or high-fat meal (approximately 800 kcal, 50% fat) resulted in 
increased exposures of elvitegravir.  The Cmax and AUCtau of elvitegravir increased 22% and 36% with 
a light meal, while increasing 56% and 91% with a high-fat meal, respectively. 
 
Distribution 
Elvitegravir is 98-99% bound to human plasma proteins and the binding is independent of drug 
concentration over the range of 1.0 ng/mL to 1.6 µg/mL.  The mean plasma to blood drug 
concentration ratio is 1.37. 
 
Biotransformation 
Elvitegravir undergoes oxidative metabolism by CYP3A (major route), and glucuronidation via 
UGT1A1/3 enzymes (minor route). 
 
Ritonavir inhibits CYP3A, thereby substantially increasing the plasma concentrations of elvitegravir.  
Administration of once-daily ritonavir (20-200 mg) results in an increased elvitegravir exposure 
following repeat once-daily administration, with elvitegravir exposure reaching a plateau with 
approximately 100 mg of ritonavir.  Further increases in ritonavir dose do not result in further 
increases in elvitegravir exposure.  Vitekta is indicated for use only when co-administered with 
ritonavir as a boosting agent. 
 
Mean steady-state exposure (AUCtau) of unboosted elvitegravir is ~ 20% lower after multiple dosing 
versus a single dose, indicating modest autoinduction of its metabolism.  Upon boosting with ritonavir 
(100 mg), net inhibition of elvitegravir metabolism is observed with significantly increased systemic 
exposures (20-fold higher AUC), high trough concentrations, and longer median elimination half-life 
(9.5 versus 3.5 hours). 
 

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Following oral administration of a single dose of ritonavir-boosted [14C]elvitegravir, elvitegravir was 
the predominant species in plasma, representing approximately 94% and 61% of the circulating 
radioactivity at 32 and 48 hours, respectively.  Metabolites produced by aromatic and aliphatic 
hydroxylation or glucuronidation are present in very low levels and do not contribute to the overall 
antiviral activity of elvitegravir. 
 
Elimination 
Following oral administration of ritonavir-boosted [14C]elvitegravir, 94.8% of the dose was recovered 
in faeces, consistent with the hepatobiliary elimination of elvitegravir; 6.7% of the administered dose 
was recovered in urine as metabolites.  The median terminal plasma half-life of ritonavir-boosted 
elvitegravir is approximately 8.7 to 13.7 hours. 
 
Linearity/non-linearity 
Elvitegravir plasma exposures are non-linear and less than dose-proportional, likely due to solubility-
limited absorption. 
 
Elderly 
Pharmacokinetics of elvitegravir have not been fully evaluated in the elderly (over 65 years of age). 
 
Gender 
No clinically relevant pharmacokinetic differences due to gender have been identified for boosted 
elvitegravir. 
 
Ethnicity 
No clinically relevant pharmacokinetic differences due to ethnicity have been identified for boosted 
elvitegravir. 
 
Paediatric population 
The pharmacokinetics of elvitegravir in paediatric subjects have not been established. 
 
Renal impairment 
A study of the pharmacokinetics of boosted elvitegravir was performed in non HIV-1 infected subjects 
with severe renal impairment (estimated creatinine clearance below 30 mL/min).  No clinically 
relevant differences in elvitegravir pharmacokinetics were observed between subjects with severe 
renal impairment and healthy subjects.  No dose adjustment of Vitekta is required for patients with 
renal impairment. 
 
Hepatic impairment 
Elvitegravir is primarily metabolised and eliminated by the liver.  A study of the pharmacokinetics of 
boosted elvitegravir was performed in non-HIV-1 infected subjects with moderate hepatic impairment 
(Child-Pugh Class B).  No clinically relevant differences in elvitegravir pharmacokinetics were 
observed between subjects with moderate impairment and healthy subjects.  No dose adjustment of 
Vitekta is necessary for patients with mild to moderate hepatic impairment.  The effect of severe 
hepatic impairment (Child-Pugh Class C) on the pharmacokinetics of elvitegravir has not been studied. 
 
Hepatitis B and/or hepatitis C virus co-infection 
Limited data from population pharmacokinetic analysis (n = 56) indicated that hepatitis B and/or 
C virus infection had no clinically relevant effect on the exposure of boosted elvitegravir. 
 
5.3 Preclinical safety data 
 
Non-clinical data reveal no special hazard for humans based on conventional studies of safety 
pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, toxicity to reproduction 
and development.  The maximum doses of elvitegravir tested in the development toxicity studies in 
rats and rabbits corresponded to exposures that are approximately 29-fold and 0.2-fold the human 
therapeutic exposure, respectively. 
 

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Elvitegravir was negative in an in vitro bacterial mutagenicity test (Ames test) and negative in an 
in vivo rat micronucleus assay at doses up to 2,000 mg/kg.  In an in vitro chromosomal aberration test, 
elvitegravir was negative with metabolic activation; however, an equivocal response was observed 
without activation. 
 
Elvitegravir did not show any carcinogenic potential in long-term oral carcinogenicity studies in mice 
and rats. 
 
The active substance elvitegravir is persistent in the environment. 
 
 
6. PHARMACEUTICAL PARTICULARS 
 
6.1 List of excipients 
 
Tablet core 
Croscarmellose sodium 
Hydroxypropyl cellulose 
Lactose monohydrate 
Magnesium stearate 
Microcrystalline cellulose 
Sodium lauryl sulfate 
 
Film-coating 
Indigo carmine aluminium lake (E132) 
Macrogol 3350 (E1521) 
Polyvinyl alcohol (partially hydrolysed) (E1203) 
Talc (E553B) 
Titanium dioxide (E171) 
Iron oxide yellow (E172) 
 
6.2 Incompatibilities 
 
Not applicable. 
 
6.3 Shelf life 
 
4 years. 
 
6.4 Special precautions for storage 
 
This medicinal product does not require any special storage conditions. 
 
6.5 Nature and contents of container 
 
High density polyethylene (HDPE) bottle with a child-resistant closure containing 30 film-coated 
tablets. 
 
Pack size: 1 bottle of 30 film-coated tablets. 
 
6.6 Special precautions for disposal 
 
Any unused medicinal product or waste material should be disposed of in accordance with local 
requirements. 
 
 

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41 

7. MARKETING AUTHORISATION HOLDER 
 
Gilead Sciences International Limited 
Cambridge 
CB21 6GT 
United Kingdom 
 
 
8. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/13/883/002 
 
 
9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION 
 
Date of first authorisation: 13 November 2013 
 
 
10. DATE OF REVISION OF THE TEXT 
 
 
Detailed information on this medicinal product is available on the website of the European Medicines 
Agency http://www.ema.europa.eu. 

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42 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

ANNEX II 
 

A. MANUFACTURER(S) RESPONSIBLE FOR BATCH 
RELEASE 

 
B. CONDITIONS OR RESTRICTIONS REGARDING SUPPLY 

AND USE 
 
C. OTHER CONDITIONS AND REQUIREMENTS OF THE 

MARKETING AUTHORISATION 
 
D. CONDITIONS OR RESTRICTIONS WITH REGARD TO 

THE SAFE AND EFFECTIVE USE OF THE MEDICINAL 
PRODUCT 

 
 

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A. MANUFACTURER(S) RESPONSIBLE FOR BATCH RELEASE 
 
Name and address of the manufacturer(s) responsible for batch release 
 
Gilead Sciences Ireland UC 
IDA Business & Technology Park 
Carrigtohill 
County Cork 
Ireland 
 
 
B. CONDITIONS OR RESTRICTIONS REGARDING SUPPLY AND USE 
 
Medicinal product subject to restricted medical prescription (see Annex I: Summary of Product 
Characteristics, section 4.2). 
 
 
C. OTHER CONDITIONS AND REQUIREMENTS OF THE 

MARKETING AUTHORISATION 
 
• Periodic Safety Update Reports 
 
The marketing authorisation holder shall submit the first periodic safety update report for this product 
within 6 months following authorisation.  Subsequently, the marketing authorisation holder shall 
submit periodic safety update reports for this product in accordance with the requirements set out in 
the list of Union reference dates (EURD list) provided for under Article 107c(7) of 
Directive 2001/83/EC and published on the European medicines web-portal. 
 
 
D. CONDITIONS OR RESTRICTIONS WITH REGARD TO THE SAFE 

AND EFFECTIVE USE OF THE MEDICINAL PRODUCT 
 
• Risk Management Plan (RMP) 
 
The MAH shall perform the required pharmacovigilance activities and interventions detailed in the 
agreed RMP presented in Module 1.8.2 of the Marketing Authorisation and any agreed subsequent 
updates of the RMP. 
 
An updated RMP should be submitted: 
• At the request of the European Medicines Agency; 
• Whenever the risk management system is modified, especially as the result of new information 

being received that may lead to a significant change to the benefit/risk profile or as the result of 
an important (pharmacovigilance or risk minimisation) milestone being reached. 

 
If the dates for submission of a PSUR and the update of a RMP coincide, they can be submitted at the 
same time. 
 

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44 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

ANNEX III 
 

LABELLING AND PACKAGE LEAFLET 

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A. LABELLING 

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PARTICULARS TO APPEAR ON THE OUTER PACKAGING AND THE IMMEDIATE 
PACKAGING 
 
BOTTLE AND CARTON LABELLING 
 
1. NAME OF THE MEDICINAL PRODUCT 
 
Vitekta 85 mg film-coated tablets 
Elvitegravir 
 
 
2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each film-coated tablet contains 85 mg of elvitegravir. 
 
 
3. LIST OF EXCIPIENTS 
 
Contains lactose, see leaflet for further information. 
 
 
4. PHARMACEUTICAL FORM AND CONTENTS 
 
30 film-coated tablets. 
30 tablets. 
 
 
5. METHOD AND ROUTE(S) OF ADMINISTRATION 
 
Read the package leaflet before use. 
 
Oral use. 
 
 
6. SPECIAL WARNING THAT THE MEDICINAL PRODUCT MUST BE STORED OUT 

OF THE SIGHT AND REACH OF CHILDREN 
 
Keep out of the sight and reach of children. 
 
 
7. OTHER SPECIAL WARNING(S), IF NECESSARY 
 
 
8. EXPIRY DATE 
 
EXP 
 
 
9. SPECIAL STORAGE CONDITIONS 
 
 

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10. SPECIAL PRECAUTIONS FOR DISPOSAL OF UNUSED MEDICINAL PRODUCTS 
OR WASTE MATERIALS DERIVED FROM SUCH MEDICINAL PRODUCTS, IF 
APPROPRIATE 

 
 
11. NAME AND ADDRESS OF THE MARKETING AUTHORISATION HOLDER 
 
Gilead Sciences Intl Ltd 
Cambridge 
CB21 6GT 
United Kingdom 
 
 
12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/13/883/001 
 
 
13. BATCH NUMBER 
 
Lot 
 
 
14. GENERAL CLASSIFICATION FOR SUPPLY 
 
Medicinal product subject to medical prescription. 
 
 
15. INSTRUCTIONS ON USE 
 
 
16. INFORMATION IN BRAILLE 
 
Vitekta 85 mg [Outer packaging only] 

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PARTICULARS TO APPEAR ON THE OUTER PACKAGING AND THE IMMEDIATE 
PACKAGING 
 
BOTTLE AND CARTON LABELLING 
 
1. NAME OF THE MEDICINAL PRODUCT 
 
Vitekta 150 mg film-coated tablets 
Elvitegravir 
 
 
2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each film-coated tablet contains 150 mg of elvitegravir. 
 
 
3. LIST OF EXCIPIENTS 
 
Contains lactose, see leaflet for further information. 
 
 
4. PHARMACEUTICAL FORM AND CONTENTS 
 
30 film-coated tablets. 
30 tablets. 
 
 
5. METHOD AND ROUTE(S) OF ADMINISTRATION 
 
Read the package leaflet before use. 
 
Oral use. 
 
 
6. SPECIAL WARNING THAT THE MEDICINAL PRODUCT MUST BE STORED OUT 

OF THE SIGHT AND REACH OF CHILDREN 
 
Keep out of the sight and reach of children. 
 
 
7. OTHER SPECIAL WARNING(S), IF NECESSARY 
 
 
8. EXPIRY DATE 
 
EXP 
 
 
9. SPECIAL STORAGE CONDITIONS 
 
 

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10. SPECIAL PRECAUTIONS FOR DISPOSAL OF UNUSED MEDICINAL PRODUCTS 
OR WASTE MATERIALS DERIVED FROM SUCH MEDICINAL PRODUCTS, IF 
APPROPRIATE 

 
 
11. NAME AND ADDRESS OF THE MARKETING AUTHORISATION HOLDER 
 
Gilead Sciences Intl Ltd 
Cambridge 
CB21 6GT 
United Kingdom 
 
 
12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/13/883/002 
 
 
13. BATCH NUMBER 
 
Lot 
 
 
14. GENERAL CLASSIFICATION FOR SUPPLY 
 
Medicinal product subject to medical prescription. 
 
 
15. INSTRUCTIONS ON USE 
 
 
16. INFORMATION IN BRAILLE 
 
Vitekta 150 mg [Outer packaging only] 

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50 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

B. PACKAGE LEAFLET 

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Package leaflet: Information for the patient 
 

Vitekta 85 mg film-coated tablets 
Elvitegravir 

 
This medicine is subject to additional monitoring.  This will allow quick identification of new 

safety information.  You can help by reporting any side effects you may get.  See the end of section 4 
for how to report side effects. 
 
Read all of this leaflet carefully before you start taking this medicine because it contains 
important information for you. 
- Keep this leaflet.  You may need to read it again. 
- If you have any further questions, ask your doctor or pharmacist. 
- This medicine has been prescribed for you only.  Do not pass it on to others.  It may harm them, 

even if their signs of illness are the same as yours. 
- If you get any side effects talk to your doctor or pharmacist.  This includes any possible side 

effects not listed in this leaflet.  See section 4. 
 
What is in this leaflet 
 
1. What Vitekta is and what it is used for 
2. What you need to know before you take Vitekta 
3. How to take Vitekta 
4. Possible side effects 
5. How to store Vitekta 
6. Contents of the pack and other information 
 
 
1. What Vitekta is and what it is used for 
 
Vitekta contains the active substance elvitegravir. 
 
Vitekta is a treatment for human immunodeficiency virus (HIV) infection in adults aged 18 years 
and over. 
 
Vitekta must always be taken with certain other HIV medicines.  See section 3, How to take 
Vitekta. 
 
The HIV virus produces an enzyme called HIV integrase.  This enzyme helps the virus to multiply in 
the cells in your body.  Vitekta stops this enzyme working and reduces the amount of HIV in your 
body.  This will improve your immune system and reduce the risk of developing illnesses linked to 
HIV infection. 
 
This medicine is not a cure for HIV infection.  While taking Vitekta you may still develop infections 
or other illnesses associated with HIV infection. 
 
 
2. What you need to know before you take Vitekta 
 
Do not take Vitekta 
 
• if you are allergic to elvitegravir or any of the other ingredients of this medicine (listed in 

section 6 of this leaflet). 
 

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• if you are taking one of these medicines: 
- carbamazepine, phenobarbital, phenytoin, used to treat epilepsy and prevent seizures 
- rifampicin, used to prevent and treat tuberculosis and other infections 
- St. John’s wort (Hypericum perforatum), a herbal remedy used for depression and 

anxiety, or products that contain it 
 
 If any of these applies to you, do not take Vitekta and tell your doctor immediately. 
 
Warnings and precautions 
 
Your treatment with Vitekta should only be started by a doctor who is experienced in treating 
HIV infection. 
 
You can still pass on HIV when taking this medicine, although the risk is lowered by effective 
antiretroviral therapy.  Discuss with your doctor the precautions needed to avoid infecting other 
people.  This medicine is not a cure for HIV infection.  While taking Vitekta you may still develop 
infections or other illnesses associated with HIV infection. 
 
Talk to your doctor before taking Vitekta: 
 
• If you have liver problems or a history of liver disease, including hepatitis.  Patients with 

liver disease including chronic hepatitis B or C, who are treated with antiretrovirals, have a 
higher risk of severe and potentially fatal liver complications.  If you have hepatitis B infection, 
your doctor will carefully consider the best treatment for you. 

 
 If any of these applies to you, talk to your doctor before taking Vitekta. 
 
While you are taking Vitekta 
 
Look out for the following: 
 
• any signs of inflammation or infection 
 
• bone problems 
 
 If you notice any of these symptoms, tell your doctor immediately.  For more information see 

section 4 of this leaflet. 
 
Children and adolescents 
 
• Do not give this medicine to children and adolescents under 18 years of age.  The use of 

Vitekta in children and adolescents has not yet been studied. 
 
Other medicines and Vitekta 
 
Tell your doctor or pharmacist if you are taking, plan to take, or have recently taken any other 
medicines.  This includes medicines and herbal products obtained without a prescription.  Vitekta may 
interact with other medicines which can affect the amounts of Vitekta or other medicines in your 
blood.  This may stop your medicines from working properly, or may make any side effects worse. 
 
Medicines that should never be taken with Vitekta: 
• carbamazepine, phenobarbital, phenytoin, used to treat epilepsy and prevent seizures 
• rifampicin, used to prevent and treat tuberculosis and other infections 
• St. John’s wort (Hypericum perforatum), a herbal remedy used for depression and anxiety, or 

products that contain it 
 

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Other medicines used in treating HIV infection: 
You should not take Vitekta with other medicines containing: 
• cobicistat 
• elvitegravir 
 
Talk to your doctor if you are taking: 
• efavirenz 
• nevirapine 
• didanosine (see also section 3 of this leaflet) 
 Tell your doctor if you are taking any of these HIV medicines. 
 
Other types of medicine: 
Talk to your doctor if you are taking: 
• rifabutin, used to treat bacterial infections including tuberculosis 
• warfarin, used to thin the blood 
• contraceptive pill, used to prevent pregnancy 
• bosentan, used to treat pulmonary arterial hypertension 
• antacids, used to treat heartburn or acid reflux, such as aluminium/magnesium hydroxide or 

calcium carbonate (see also section 3 of this leaflet) 
• multivitamins, used to supplement your diet (see also section 3 of this leaflet). 
 Tell your doctor if any of these apply to you. 
 
 Tell your doctor if you are taking these or any other medicines.  Do not stop your treatment 

without contacting your doctor. 
 
Pregnancy and breast-feeding 
 
Ask your doctor or pharmacist for advice before taking any medicine. 
 
• Women must not get pregnant while taking Vitekta. 
• Use effective contraception while taking Vitekta. 
• Tell your doctor immediately if you become pregnant.  If you are pregnant, you should not 

take Vitekta unless you and your doctor decide it is clearly needed.  Your doctor will discuss the 
potential benefits and risks of taking Vitekta to you and your child. 

 
Do not breast-feed during treatment with Vitekta: It is not known if the active substance in this 
medicine can pass into human breast milk.  If you are a woman with HIV it is recommended that you 
do not breast-feed to avoid passing the virus to the baby in breast milk. 
 
Vitekta contains lactose 
 
Tell your doctor if you are lactose intolerant or intolerant to other sugars.  Vitekta contains 
lactose.  If you are lactose-intolerant, or if you have been told that you have an intolerance to other 
sugars, talk to your doctor before taking this medicine. 
 
 
3. How to take Vitekta 
 
Always take this medicine exactly as your doctor has told you.  Check with your doctor or pharmacist 
if you are not sure.  This is to make sure that your medicine is fully effective, and to reduce the risk of 
developing resistance to the treatment.  Do not change the dose unless your doctor tells you to. 
 
You must always take Vitekta with one of the following combinations of medicines: 
 
• atazanavir and ritonavir 
• darunavir and ritonavir 

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• fosamprenavir and ritonavir 
• lopinavir/ritonavir 
 
A dose of 85 mg is recommended: 
If you are taking Vitekta with: 
• atazanavir and ritonavir 
• lopinavir/ritonavir 
 
In these combinations the dose is one 85 mg tablet each day, with food.  Do not chew, crush or 
split the tablet.  Take the 85 mg tablet at the same time as atazanavir and ritonavir, or at the same time 
as the first dose of lopinavir/ritonavir. 
 
A dose of 150 mg is recommended: 
If you are taking Vitekta with: 
• darunavir and ritonavir 
• fosamprenavir and ritonavir 
 
In these combinations the dose is one 150 mg tablet each day, with food.  Do not chew, crush or 
split the tablet.  Take the 150 mg tablet at the same time as the first dose of darunavir or fosamprenavir 
and ritonavir.  Refer to the package leaflet for Vitekta 150 mg tablets. 
 
If you are also taking other medicines: 
 
If you are also taking didanosine, take it at least 1 hour before or at least 2 hours after Vitekta. 
 
If you are also taking an antacid such as aluminium/magnesium hydroxide or calcium carbonate, or 
a multivitamin supplement, take it at least 4 hours before or at least 4 hours after Vitekta. 
 
If you take more Vitekta than you should 
 
If you accidentally take more than the recommended dose of Vitekta you may be at increased risk of 
experiencing possible side effects with this medicine (see section 4 of this leaflet). 
 
Contact your doctor or nearest emergency department immediately for advice.  Keep the tablet bottle 
with you so that you can easily describe what you have taken. 
 
If you forget to take Vitekta 
 
It is important not to miss a dose of Vitekta. 
 
If you do miss a dose: 
• If you notice within 18 hours of the time you usually take Vitekta, you must take the tablet as 

soon as possible.  Always take the tablet with food.  Then take the next dose as usual. 
• If you notice 18 hours or more after the time you usually take Vitekta, then do not take the 

missed dose.  Wait and take the next dose, with food, at your usual time. 
 
If you vomit less than 1 hour after taking Vitekta, take another tablet with food. 
 
Do not stop taking Vitekta 
 
Do not stop taking Vitekta without talking to your doctor.  Stopping Vitekta can seriously affect 
your response to future treatment.  If Vitekta is stopped for any reason, speak to your doctor before 
you restart taking Vitekta tablets. 
 
When your supply of Vitekta starts to run low, get more from your doctor or pharmacist.  This is 
very important because the amount of virus may start to increase if the medicine is stopped for even a 
short time.  The disease may then become harder to treat. 

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If you have any further questions on the use of this medicine, ask your doctor or pharmacist. 
 
 
4. Possible side effects 
 
During HIV therapy there may be an increase in weight and in levels of blood lipids and glucose.  This 
is partly linked to restored health and life style, and in the case of blood lipids sometimes to the HIV 
medicines themselves.  Your doctor will test for these changes. 
 
Like all medicines, this medicine can cause side effects, although not everybody gets them.  When 
treating HIV infection, it is not always possible to tell whether some of the unwanted effects are 
caused by Vitekta or by other medicines that you are taking at the same time, or by the HIV infection 
itself. 
 
Common side effects 
(may affect 1 to 10 in every 100 patients treated) 
• stomach pain 
• vomiting 
• rashes 
• headache 
• diarrhoea 
• feeling sick (nausea) 
• tiredness. 
 
Uncommon side effects 
(may affect up to 1 in every 100 patients treated) 
• suicidal thoughts and suicide attempts (in patients who have had depression or mental health 

problems before) 
• depression 
• difficulty sleeping (insomnia) 
• problems with digestion resulting in discomfort after meals (dyspepsia) 
• feeling bloated 
• wind (flatulence) 
• dizziness 
• tingling 
• sleepiness 
• abnormal taste. 
 
 If you think that you may have any of these side effects, talk to your doctor. 
 
Other effects that may be seen during HIV treatment 
The frequency of the following side effects is not known (frequency cannot be estimated from the 
available data): 
 
• Any signs of inflammation or infection.  If you have advanced HIV infection (AIDS) and 

have an infection, you may develop symptoms of infection and inflammation or worsening of 
the symptoms of an existing infection once treatment with Vitekta is started.  These symptoms 
may indicate that your body’s improved immune system is fighting infection.  Look out for 
signs of inflammation or infection soon after you start taking Vitekta.  If you notice signs of 
inflammation or infection, tell your doctor at once.  In addition to the opportunistic infections, 
autoimmune disorders (a condition that occurs when the immune system attacks healthy body 
tissue) may also occur after you start taking medicines for the treatment of your HIV infection.  
Autoimmune disorders may occur many months after the start of treatment.  If you notice any 
symptoms of infection or other symptoms such as muscle weakness, weakness beginning in the 

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hands and feet and moving up towards the trunk of the body, palpitations, tremor or 
hyperactivity, please inform your doctor immediately to seek necessary treatment. 

 
• Bone problems.  Some patients taking combination antiretroviral therapy may develop a bone 

disease called osteonecrosis (death of bone tissue caused by loss of blood supply to the bone).  
The length of combination antiretroviral therapy, corticosteroid use, alcohol consumption, 
severe immunosuppression, higher body mass index, among others, may be some of the many 
risk factors for developing this disease.  Signs of osteonecrosis are: 
- joint stiffness 
- joint aches and pains (especially of the hip, knee and shoulder) 
- difficulty with movement. 
If you notice any of these symptoms, tell your doctor. 

 
Reporting of side effects 
 If you get any side effects, talk to your doctor or pharmacist.  This includes any possible side 

effects not listed in this leaflet.  You can also report side effects directly via the national reporting 
system listed in Appendix V.  By reporting side effects you can help provide more information on 
the safety of this medicine. 

 
 
5. How to store Vitekta 
 
Keep this medicine out of the sight and reach of children. 
 
Do not use this medicine after the expiry date which is stated on the bottle and carton after {EXP}.  
The expiry date refers to the last day of that month. 
 
This medicine does not require any special storage conditions. 
 
Do not throw away any medicines via wastewater or household waste.  Ask your pharmacist how to 
throw away medicines you no longer use.  These measures will help protect the environment. 
 
 
6. Contents of the pack and other information 
 
What Vitekta contains 
 
The active substance is elvitegravir.  Each film-coated tablet contains 85 mg elvitegravir. 
 
The other ingredients are 
 
Tablet core: 
Croscarmellose sodium, hydroxypropyl cellulose, lactose (as monohydrate), magnesium stearate, 
microcrystalline cellulose, sodium lauryl sulfate. 
 
Film-coating: 
Indigo carmine aluminium lake (E132), macrogol 3350 (E1521), polyvinyl alcohol (partially 
hydrolysed) (E1203), talc (E553B), titanium dioxide (E171), iron oxide yellow (E172). 
 
What Vitekta looks like and contents of the pack 
 
Vitekta film-coated tablets are green, pentagon-shaped tablets, debossed on one side with “GSI” and 
“85” on the other side of the tablet. 
 
The following pack size is available: outer cartons containing 1 bottle of 30 film-coated tablets. 
 

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http://www.ema.europa.eu/docs/en_GB/document_library/Template_or_form/2013/03/WC500139752.doc


57 

Marketing Authorisation Holder 
Gilead Sciences International Limited 
Cambridge 
CB21 6GT 
United Kingdom 
 
Manufacturer 
Gilead Sciences Ireland UC 
IDA Business & Technology Park 
Carrigtohill 
County Cork 
Ireland 
 
For any information about this medicine, please contact the local representative of the Marketing 
Authorisation Holder: 
 
België/Belgique/Belgien 
Gilead Sciences Belgium SPRL-BVBA 
Tél/Tel: + 32 (0) 24 01 35 50 
 

Lietuva 
Gilead Sciences Sweden AB 
Tel: + 46 (0) 8 5057 1849 
 

България 
Gilead Sciences International Ltd 
Тел.: + 44 (0) 20 7136 8820 
 

Luxembourg/Luxemburg 
Gilead Sciences Belgium SPRL-BVBA 
Tél/Tel: + 32 (0) 24 01 35 50 
 

Česká republika 
Gilead Sciences s.r.o. 
Tel: + 420 222 191 546 
 

Magyarország 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

Danmark 
Gilead Sciences Sweden AB 
Tlf: + 46 (0) 8 5057 1849 
 

Malta 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

Deutschland 
Gilead Sciences GmbH 
Tel: + 49 (0) 89 899890-0 
 

Nederland 
Gilead Sciences Netherlands B.V. 
Tel: + 31 (0) 20 718 36 98 
 

Eesti 
Gilead Sciences Sweden AB 
Tel: + 46 (0) 8 5057 1849 
 

Norge 
Gilead Sciences Sweden AB 
Tlf: + 46 (0) 8 5057 1849 
 

Ελλάδα 
Gilead Sciences Ελλάς Μ.ΕΠΕ. 
Τηλ: + 30 210 8930 100 
 

Österreich 
Gilead Sciences GesmbH 
Tel: + 43 1 260 830 
 

España 
Gilead Sciences, S.L. 
Tel: + 34 91 378 98 30 
 

Polska 
Gilead Sciences Poland Sp. z o.o. 
Tel: +48 22 262 8702 
 

France 
Gilead Sciences 
Tél: + 33 (0) 1 46 09 41 00 
 

Portugal 
Gilead Sciences, Lda. 
Tel: + 351 21 7928790 
 

Hrvatska 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

România 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

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Ireland 
Gilead Sciences Ltd 
Tel: + 44 (0) 8000 113 700 
 

Slovenija 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

Ísland 
Gilead Sciences Sweden AB 
Sími: + 46 (0) 8 5057 1849 
 

Slovenská republika 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

Italia 
Gilead Sciences S.r.l. 
Tel: + 39 02 439201 
 

Suomi/Finland 
Gilead Sciences Sweden AB 
Puh/Tel: + 46 (0) 8 5057 1849 
 

Κύπρος 
Gilead Sciences Ελλάς Μ.ΕΠΕ. 
Τηλ: + 30 210 8930 100 
 

Sverige 
Gilead Sciences Sweden AB 
Tel: + 46 (0) 8 5057 1849 
 

Latvija 
Gilead Sciences Sweden AB 
Tel: + 46 (0) 8 5057 1849 
 

United Kingdom 
Gilead Sciences Ltd 
Tel: + 44 (0) 8000 113 700 
 

 
This leaflet was last revised in {MM/YYYY}. 
 
Detailed information on this medicine is available on the European Medicines Agency web site: 
http://www.ema.europa.eu. 

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59 

Package leaflet: Information for the patient 
 

Vitekta 150 mg film-coated tablets 
Elvitegravir 

 
This medicine is subject to additional monitoring.  This will allow quick identification of new 

safety information.  You can help by reporting any side effects you may get.  See the end of section 4 
for how to report side effects. 
 
Read all of this leaflet carefully before you start taking this medicine because it contains 
important information for you. 
- Keep this leaflet.  You may need to read it again. 
- If you have any further questions, ask your doctor or pharmacist. 
- This medicine has been prescribed for you only.  Do not pass it on to others.  It may harm them, 

even if their signs of illness are the same as yours. 
- If you get any side effects talk to your doctor or pharmacist.  This includes any possible side 

effects not listed in this leaflet.  See section 4. 
 
What is in this leaflet 
 
1. What Vitekta is and what it is used for 
2. What you need to know before you take Vitekta 
3. How to take Vitekta 
4. Possible side effects 
5. How to store Vitekta 
6. Contents of the pack and other information 
 
 
1. What Vitekta is and what it is used for 
 
Vitekta contains the active substance elvitegravir. 
 
Vitekta is a treatment for human immunodeficiency virus (HIV) infection in adults aged 18 years 
and over. 
 
Vitekta must always be taken with certain other HIV medicines.  See section 3, How to take 
Vitekta. 
 
The HIV virus produces an enzyme called HIV integrase.  This enzyme helps the virus to multiply in 
the cells in your body.  Vitekta stops this enzyme working and reduces the amount of HIV in your 
body.  This will improve your immune system and reduce the risk of developing illnesses linked to 
HIV infection. 
 
This medicine is not a cure for HIV infection.  While taking Vitekta you may still develop infections 
or other illnesses associated with HIV infection. 
 
 
2. What you need to know before you take Vitekta 
 
Do not take Vitekta 
 
• if you are allergic to elvitegravir or any of the other ingredients of this medicine (listed in 

section 6 of this leaflet). 
 

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• if you are taking one of these medicines: 
- carbamazepine, phenobarbital, phenytoin, used to treat epilepsy and prevent seizures 
- rifampicin, used to prevent and treat tuberculosis and other infections 
- St. John’s wort (Hypericum perforatum), a herbal remedy used for depression and 

anxiety, or products that contain it 
 
 If any of these applies to you, do not take Vitekta and tell your doctor immediately. 
 
Warnings and precautions 
 
Your treatment with Vitekta should only be started by a doctor who is experienced in treating 
HIV infection. 
 
You can still pass on HIV when taking this medicine, although the risk is lowered by effective 
antiretroviral therapy.  Discuss with your doctor the precautions needed to avoid infecting other 
people.  This medicine is not a cure for HIV infection.  While taking Vitekta you may still develop 
infections or other illnesses associated with HIV infection. 
 
Talk to your doctor before taking Vitekta: 
 
• If you have liver problems or a history of liver disease, including hepatitis.  Patients with 

liver disease including chronic hepatitis B or C, who are treated with antiretrovirals, have a 
higher risk of severe and potentially fatal liver complications.  If you have hepatitis B infection, 
your doctor will carefully consider the best treatment for you. 

 
 If any of these applies to you, talk to your doctor before taking Vitekta. 
 
While you are taking Vitekta 
 
Look out for the following: 
 
• any signs of inflammation or infection 
 
• bone problems 
 
 If you notice any of these symptoms, tell your doctor immediately.  For more information see 

section 4 of this leaflet. 
 
Children and adolescents 
 
• Do not give this medicine to children and adolescents under 18 years of age.  The use of 

Vitekta in children and adolescents has not yet been studied. 
 
Other medicines and Vitekta 
 
Tell your doctor or pharmacist if you are taking, plan to take, or have recently taken any other 
medicines.  This includes medicines and herbal products obtained without a prescription.  Vitekta may 
interact with other medicines which can affect the amounts of Vitekta or other medicines in your 
blood.  This may stop your medicines from working properly, or may make any side effects worse. 
 
Medicines that should never be taken with Vitekta: 
• carbamazepine, phenobarbital, phenytoin, used to treat epilepsy and prevent seizures 
• rifampicin, used to prevent and treat tuberculosis and other infections 
• St. John’s wort (Hypericum perforatum), a herbal remedy used for depression and anxiety, or 

products that contain it 
 

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Other medicines used in treating HIV infection: 
You should not take Vitekta with other medicines containing: 
• cobicistat 
• elvitegravir 
 
Talk to your doctor if you are taking: 
• efavirenz 
• nevirapine 
• didanosine (see also section 3 of this leaflet) 
 Tell your doctor if you are taking any of these HIV medicines. 
 
Other types of medicine: 
Talk to your doctor if you are taking: 
• rifabutin, used to treat bacterial infections including tuberculosis 
• warfarin, used to thin the blood 
• contraceptive pill, used to prevent pregnancy 
• bosentan, used to treat pulmonary arterial hypertension 
• antacids, used to treat heartburn or acid reflux, such as aluminium/magnesium hydroxide or 

calcium carbonate (see also section 3 of this leaflet) 
• multivitamins, used to supplement your diet (see also section 3 of this leaflet). 
 Tell your doctor if any of these apply to you. 
 
 Tell your doctor if you are taking these or any other medicines.  Do not stop your treatment 

without contacting your doctor. 
 
Pregnancy and breast-feeding 
 
Ask your doctor or pharmacist for advice before taking any medicine. 
 
• Women must not get pregnant while taking Vitekta. 
• Use effective contraception while taking Vitekta. 
• Tell your doctor immediately if you become pregnant.  If you are pregnant, you should not 

take Vitekta unless you and your doctor decide it is clearly needed.  Your doctor will discuss the 
potential benefits and risks of taking Vitekta to you and your child. 

 
Do not breast-feed during treatment with Vitekta: It is not known if the active substance in this 
medicine can pass into human breast milk.  If you are a woman with HIV it is recommended that you 
do not breast-feed to avoid passing the virus to the baby in breast milk. 
 
Vitekta contains lactose 
 
Tell your doctor if you are lactose intolerant or intolerant to other sugars.  Vitekta contains 
lactose.  If you are lactose-intolerant, or if you have been told that you have an intolerance to other 
sugars, talk to your doctor before taking this medicine. 
 
 
3. How to take Vitekta 
 
Always take this medicine exactly as your doctor has told you.  Check with your doctor or pharmacist 
if you are not sure.  This is to make sure that your medicine is fully effective, and to reduce the risk of 
developing resistance to the treatment.  Do not change the dose unless your doctor tells you to. 
 
You must always take Vitekta with one of the following combinations of medicines: 
 
• atazanavir and ritonavir 
• darunavir and ritonavir 

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• fosamprenavir and ritonavir 
• lopinavir/ritonavir 
 
A dose of 150 mg is recommended: 
If you are taking Vitekta with: 
• darunavir and ritonavir 
• fosamprenavir and ritonavir 
 
In these combinations the dose is one 150 mg tablet each day, with food.  Do not chew, crush or 
split the tablet.  Take the 150 mg tablet at the same time as the first dose of darunavir or fosamprenavir 
and ritonavir. 
 
A dose of 85 mg is recommended: 
If you are taking Vitekta with: 
• atazanavir and ritonavir 
• lopinavir/ritonavir 
 
In these combinations the dose is one 85 mg tablet each day, with food.  Do not chew, crush or 
split the tablet.  Take the 85 mg tablet at the same time as atazanavir and ritonavir, or at the same time 
as the first dose of lopinavir/ritonavir.  Refer to the package leaflet for Vitekta 85 mg tablets. 
 
If you are also taking other medicines: 
 
If you are also taking didanosine, take it at least 1 hour before or at least 2 hours after Vitekta. 
 
If you are also taking an antacid such as aluminium/magnesium hydroxide or calcium carbonate, or 
a multivitamin supplement, take it at least 4 hours before or at least 4 hours after Vitekta. 
 
If you take more Vitekta than you should 
 
If you accidentally take more than the recommended dose of Vitekta you may be at increased risk of 
experiencing possible side effects with this medicine (see section 4 of this leaflet). 
 
Contact your doctor or nearest emergency department immediately for advice.  Keep the tablet bottle 
with you so that you can easily describe what you have taken. 
 
If you forget to take Vitekta 
 
It is important not to miss a dose of Vitekta. 
 
If you do miss a dose: 
• If you notice within 18 hours of the time you usually take Vitekta, you must take the tablet as 

soon as possible.  Always take the tablet with food.  Then take the next dose as usual. 
• If you notice 18 hours or more after the time you usually take Vitekta, then do not take the 

missed dose.  Wait and take the next dose, with food, at your usual time. 
 
If you vomit less than 1 hour after taking Vitekta, take another tablet with food. 
 
Do not stop taking Vitekta 
 
Do not stop taking Vitekta without talking to your doctor.  Stopping Vitekta can seriously affect 
your response to future treatment.  If Vitekta is stopped for any reason, speak to your doctor before 
you restart taking Vitekta tablets. 
 
When your supply of Vitekta starts to run low, get more from your doctor or pharmacist.  This is 
very important because the amount of virus may start to increase if the medicine is stopped for even a 
short time.  The disease may then become harder to treat. 

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If you have any further questions on the use of this medicine, ask your doctor or pharmacist. 
 
 
4. Possible side effects 
 
During HIV therapy there may be an increase in weight and in levels of blood lipids and glucose.  This 
is partly linked to restored health and life style, and in the case of blood lipids sometimes to the HIV 
medicines themselves.  Your doctor will test for these changes. 
 
Like all medicines, this medicine can cause side effects, although not everybody gets them.  When 
treating HIV infection, it is not always possible to tell whether some of the unwanted effects are 
caused by Vitekta or by other medicines that you are taking at the same time, or by the HIV infection 
itself. 
 
Common side effects 
(may affect 1 to 10 in every 100 patients treated) 
• stomach pain 
• vomiting 
• rashes 
• headache 
• diarrhoea 
• feeling sick (nausea) 
• tiredness. 
 
Uncommon side effects 
(may affect up to 1 in every 100 patients treated) 
• suicidal thoughts and suicide attempts (in patients who have had depression or mental health 

problems before) 
• depression 
• difficulty sleeping (insomnia) 
• problems with digestion resulting in discomfort after meals (dyspepsia) 
• feeling bloated 
• wind (flatulence) 
• dizziness 
• tingling 
• sleepiness 
• abnormal taste. 
 
 If you think that you may have any of these side effects, talk to your doctor. 
 
Other effects that may be seen during HIV treatment 
The frequency of the following side effects is not known (frequency cannot be estimated from the 
available data): 
 
• Any signs of inflammation or infection.  If you have advanced HIV infection (AIDS) and 

have an infection, you may develop symptoms of infection and inflammation or worsening of 
the symptoms of an existing infection once treatment with Vitekta is started.  These symptoms 
may indicate that your body’s improved immune system is fighting infection.  Look out for 
signs of inflammation or infection soon after you start taking Vitekta.  If you notice signs of 
inflammation or infection, tell your doctor at once.  In addition to the opportunistic infections, 
autoimmune disorders (a condition that occurs when the immune system attacks healthy body 
tissue) may also occur after you start taking medicines for the treatment of your HIV infection.  
Autoimmune disorders may occur many months after the start of treatment.  If you notice any 
symptoms of infection or other symptoms such as muscle weakness, weakness beginning in the 

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hands and feet and moving up towards the trunk of the body, palpitations, tremor or 
hyperactivity, please inform your doctor immediately to seek necessary treatment. 

 
• Bone problems.  Some patients taking combination antiretroviral therapy may develop a bone 

disease called osteonecrosis (death of bone tissue caused by loss of blood supply to the bone).  
The length of combination antiretroviral therapy, corticosteroid use, alcohol consumption, 
severe immunosuppression, higher body mass index, among others, may be some of the many 
risk factors for developing this disease.  Signs of osteonecrosis are: 
- joint stiffness 
- joint aches and pains (especially of the hip, knee and shoulder) 
- difficulty with movement. 
If you notice any of these symptoms, tell your doctor. 

 
Reporting of side effects 
 If you get any side effects, talk to your doctor or pharmacist.  This includes any possible side 

effects not listed in this leaflet.  You can also report side effects directly via the national reporting 
system listed in Appendix V.  By reporting side effects you can help provide more information on 
the safety of this medicine. 

 
 
5. How to store Vitekta 
 
Keep this medicine out of the sight and reach of children. 
 
Do not use this medicine after the expiry date which is stated on the bottle and carton after {EXP}.  
The expiry date refers to the last day of that month. 
 
This medicine does not require any special storage conditions. 
 
Do not throw away any medicines via wastewater or household waste.  Ask your pharmacist how to 
throw away medicines you no longer use.  These measures will help protect the environment. 
 
 
6. Contents of the pack and other information 
 
What Vitekta contains 
 
The active substance is elvitegravir.  Each film-coated tablet contains 150 mg elvitegravir. 
 
The other ingredients are 
 
Tablet core: 
Croscarmellose sodium, hydroxypropyl cellulose, lactose (as monohydrate), magnesium stearate, 
microcrystalline cellulose, sodium lauryl sulfate. 
 
Film-coating: 
Indigo carmine aluminium lake (E132), macrogol 3350 (E1521), polyvinyl alcohol (partially 
hydrolysed) (E1203), talc (E553B), titanium dioxide (E171), iron oxide yellow (E172). 
 
What Vitekta looks like and contents of the pack 
 
Vitekta film-coated tablets are green, triangle-shaped tablets, debossed on one side with “GSI” and 
“150” on the other side of the tablet. 
 
The following pack size is available: outer cartons containing 1 bottle of 30 film-coated tablets. 
 

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http://www.ema.europa.eu/docs/en_GB/document_library/Template_or_form/2013/03/WC500139752.doc


65 

Marketing Authorisation Holder 
Gilead Sciences International Limited 
Cambridge 
CB21 6GT 
United Kingdom 
 
Manufacturer 
Gilead Sciences Ireland UC 
IDA Business & Technology Park 
Carrigtohill 
County Cork 
Ireland 
 
For any information about this medicine, please contact the local representative of the Marketing 
Authorisation Holder: 
 
België/Belgique/Belgien 
Gilead Sciences Belgium SPRL-BVBA 
Tél/Tel: + 32 (0) 24 01 35 50 
 

Lietuva 
Gilead Sciences Sweden AB 
Tel: + 46 (0) 8 5057 1849 
 

България 
Gilead Sciences International Ltd 
Тел.: + 44 (0) 20 7136 8820 
 

Luxembourg/Luxemburg 
Gilead Sciences Belgium SPRL-BVBA 
Tél/Tel: + 32 (0) 24 01 35 50 
 

Česká republika 
Gilead Sciences s.r.o. 
Tel: + 420 222 191 546 
 

Magyarország 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

Danmark 
Gilead Sciences Sweden AB 
Tlf: + 46 (0) 8 5057 1849 
 

Malta 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

Deutschland 
Gilead Sciences GmbH 
Tel: + 49 (0) 89 899890-0 
 

Nederland 
Gilead Sciences Netherlands B.V. 
Tel: + 31 (0) 20 718 36 98 
 

Eesti 
Gilead Sciences Sweden AB 
Tel: + 46 (0) 8 5057 1849 
 

Norge 
Gilead Sciences Sweden AB 
Tlf: + 46 (0) 8 5057 1849 
 

Ελλάδα 
Gilead Sciences Ελλάς Μ.ΕΠΕ. 
Τηλ: + 30 210 8930 100 
 

Österreich 
Gilead Sciences GesmbH 
Tel: + 43 1 260 830 
 

España 
Gilead Sciences, S.L. 
Tel: + 34 91 378 98 30 
 

Polska 
Gilead Sciences Poland Sp. z o.o. 
Tel: +48 22 262 8702 
 

France 
Gilead Sciences 
Tél: + 33 (0) 1 46 09 41 00 
 

Portugal 
Gilead Sciences, Lda. 
Tel: + 351 21 7928790 
 

Hrvatska 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

România 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

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Ireland 
Gilead Sciences Ltd 
Tel: + 44 (0) 8000 113 700 
 

Slovenija 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

Ísland 
Gilead Sciences Sweden AB 
Sími: + 46 (0) 8 5057 1849 
 

Slovenská republika 
Gilead Sciences International Ltd 
Tel: + 44 (0) 20 7136 8820 
 

Italia 
Gilead Sciences S.r.l. 
Tel: + 39 02 439201 
 

Suomi/Finland 
Gilead Sciences Sweden AB 
Puh/Tel: + 46 (0) 8 5057 1849 
 

Κύπρος 
Gilead Sciences Ελλάς Μ.ΕΠΕ. 
Τηλ: + 30 210 8930 100 
 

Sverige 
Gilead Sciences Sweden AB 
Tel: + 46 (0) 8 5057 1849 
 

Latvija 
Gilead Sciences Sweden AB 
Tel: + 46 (0) 8 5057 1849 
 

United Kingdom 
Gilead Sciences Ltd 
Tel: + 44 (0) 8000 113 700 
 

 
This leaflet was last revised in {MM/YYYY}. 
 
Detailed information on this medicine is available on the European Medicines Agency web site: 
http://www.ema.europa.eu. 
 

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	SUMMARY OF PRODUCT CHARACTERISTICS
	A. MANUFACTURER(S) RESPONSIBLE FOR BATCH RELEASE
	B. CONDITIONS OR RESTRICTIONS REGARDING SUPPLY AND USE
	C. OTHER CONDITIONS AND REQUIREMENTS OF THE MARKETING AUTHORISATION
	D. CONDITIONS OR RESTRICTIONS WITH REGARD TO THE SAFE AND EFFECTIVE USE OF THE MEDICINAL PRODUCT
	A. LABELLING
	B. PACKAGE LEAFLET