Jyseleca

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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 
 
Jyseleca 100 mg film-coated tablets 
Jyseleca 200 mg film-coated tablets 
 
 
2. QUALITATIVE AND QUANTITATIVE COMPOSITION 
 
Jyseleca 100 mg film-coated tablets 
 
Each film-coated tablet contains filgotinib maleate equivalent to 100 mg of filgotinib. 
 
Excipient with known effect 
Each 100 mg film-coated tablet contains 76 mg of lactose (as monohydrate). 
 
Jyseleca 200 mg film-coated tablets 
 
Each film-coated tablet contains filgotinib maleate equivalent to 200 mg of filgotinib. 
 
Excipient with known effect 
Each 200 mg film-coated tablet contains 152 mg of lactose (as monohydrate). 
 
For the full list of excipients, see section 6.1. 
 
 
3. PHARMACEUTICAL FORM 
 
Film-coated tablet. 
 
Jyseleca 100 mg film-coated tablets 
 
Beige 12 × 7 mm, capsule-shaped, film-coated tablet debossed with “GSI” on one side and “100” on 
the other side. 
 
Jyseleca 200 mg film-coated tablets 
 
Beige 17 × 8 mm, capsule-shaped, film-coated tablet debossed with “GSI” on one side and “200” on 
the other side. 
 
 
4. CLINICAL PARTICULARS 
 
4.1 Therapeutic indications 
 
Jyseleca is indicated for the treatment of moderate to severe active rheumatoid arthritis in adult 
patients who have responded inadequately to, or who are intolerant to one or more disease-modifying 
anti-rheumatic drugs (DMARDs). Jyseleca may be used as monotherapy or in combination with 
methotrexate (MTX). 
 



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4.2 Posology and method of administration 
 
Treatment with filgotinib should be initiated by a physician experienced in the treatment of 
rheumatoid arthritis. 
 
Posology 
 
The recommended dose of filgotinib for adult patients with rheumatoid arthritis is 200 mg once daily. 
 
Laboratory monitoring, and dose initiation or interruption 
Guidance for laboratory monitoring, and dose initiation or interruption is provided in Table 1. 
Treatment should be interrupted if a patient develops a serious infection until the infection is 
controlled (see section 4.4). 
 
Table 1: Laboratory measures and monitoring guidance 
 

Laboratory measure Action Monitoring guidance 

Absolute neutrophil count (ANC) 

Treatment should not be 
initiated, or should be 
interrupted, if ANC is 
< 1 × 109 cells/L. Treatment 
may be restarted once ANC 
returns above this value 

Before treatment initiation and 
thereafter according to routine 
patient management 

Absolute lymphocyte count 
(ALC) 

Treatment should not be 
initiated, or should be 
interrupted, if ALC is 
< 0.5 × 109 cells/L. Treatment 
may be restarted once ALC 
returns above this value 

Haemoglobin (Hb) 

Treatment should not be 
initiated, or should be 
interrupted, if Hb is < 8 g/dL. 
Treatment may be restarted 
once Hb returns above this 
value 

Lipid parameters 

Patients should be managed 
according to international 
clinical guidelines for 
hyperlipidaemia 

12 weeks after initiation of 
treatment and thereafter 
according to international 
clinical guidelines for 
hyperlipidaemia 

 
Special populations 
 
Elderly 
A starting dose of 100 mg once daily is recommended for patients aged 75 years and older as clinical 
experience is limited. 
 
Renal impairment 
No dose adjustment is required in patients with mild renal impairment (creatinine clearance 
[CrCl] ≥ 60 mL/min). A dose of 100 mg of filgotinib once daily is recommended for patients with 
moderate or severe renal impairment (CrCl 15 to < 60 mL/min). Filgotinib has not been studied in 
patients with end stage renal disease (CrCl < 15 mL/min) and is therefore not recommended for use in 
these patients (see section 5.2). 
 



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Hepatic impairment 
No dose adjustment is required in patients with mild or moderate hepatic impairment (Child-Pugh A 
or B). Filgotinib has not been studied in patients with severe hepatic impairment (Child-Pugh C) and is 
therefore not recommended for use in these patients (see section 5.2). 
 
Paediatric population 
The safety and efficacy of filgotinib in children under the age of 18 years have not yet been 
established. No data are available. 
 
Method of administration 
 
Oral use. 
Jyseleca can be taken with or without food (see section 5.2). It has not been studied if tablets can be 
split, crushed, or chewed, and it is recommended that tablets are swallowed whole. 
 
4.3 Contraindications 
 
Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. 
 
Active tuberculosis (TB) or active serious infections (see section 4.4). 
 
Pregnancy (see section 4.6). 
 
4.4 Special warnings and precautions for use 
 
Immunosuppressive medicinal products 
 
Combination of filgotinib with other potent immunosuppressants such as azathioprine, ciclosporin, 
tacrolimus, biologic DMARDs (bDMARDs) or other Janus kinase (JAK) inhibitors is not 
recommended as a risk of additive immunosuppression cannot be excluded. 
 
Infections 
 
Infections, including serious infections, have been reported in patients receiving filgotinib. The most 
frequent serious infection reported with filgotinib was pneumonia (see section 4.8). Among 
opportunistic infections, TB, oesophageal candidiasis, and cryptococcosis were reported with 
filgotinib. 
 
The risks and benefits of treatment should be considered prior to initiating filgotinib in patients: 
 
• with chronic or recurrent infection 
• who have been exposed to TB 
• with a history of a serious or an opportunistic infection 
• who have resided or travelled in areas of endemic TB or endemic mycoses; or 
• with underlying conditions that may predispose them to infection. 
 
Patients should be closely monitored for the development of signs and symptoms of infections during 
and after filgotinib treatment. If an infection develops during treatment with filgotinib, the patient 
should be carefully monitored and filgotinib treatment should be temporarily interrupted if the patient 
is not responding to standard antimicrobial therapy. Filgotinib treatment may be resumed once the 
infection is controlled. 
 
As there is a higher incidence of serious infections in the elderly aged 75 years and older, caution 
should be used when treating this population. 
 



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Tuberculosis 
Patients should be screened for TB before initiating filgotinib. Filgotinib should not be administered to 
patients with active TB (see section 4.3). In patients with latent TB, standard antimycobacterial 
therapy should be initiated before administering filgotinib. 
 
Patients should be monitored for the development of signs and symptoms of TB, including patients 
who tested negative for latent TB infection prior to initiating treatment. 
 
Viral reactivation 
 
Viral reactivation, including cases of herpes virus reactivation (e.g., herpes zoster), were reported in 
clinical studies (see section 4.8). If a patient develops herpes zoster, filgotinib treatment should be 
temporarily interrupted until the episode resolves. 
 
Screening for viral hepatitis and monitoring for reactivation should be performed in accordance with 
clinical guidelines before starting and during treatment with filgotinib. Patients who were positive for 
both hepatitis C antibody and hepatitis C virus RNA were excluded from clinical studies. Patients who 
were positive for hepatitis B surface antigen or hepatitis B virus DNA were excluded from clinical 
studies. 
 
Malignancy 
 
The risk of malignancies is increased in patients with rheumatoid arthritis. Immunomodulatory 
medicinal products may increase the risk of malignancies. The clinical data are insufficient to assess 
the potential incidence of malignancies following exposure to filgotinib. Long-term safety evaluations 
are ongoing. 
 
Malignancies were observed in clinical studies of filgotinib. The risks and benefits of filgotinib 
treatment should be considered prior to initiating treatment in patients with a known malignancy other 
than a successfully treated non-melanoma skin cancer (NMSC) or when considering continuing 
filgotinib treatment in patients who develop a malignancy. 
 
Non-melanoma skin cancer 
NMSCs have been reported in patients treated with filgotinib. Periodic skin examination is 
recommended for patients who are at increased risk for skin cancer. 
 
Fertility 
 
In animal studies, decreased fertility, impaired spermatogenesis, and histopathological effects on male 
reproductive organs were observed (see section 5.3). The potential effect of filgotinib on sperm 
production and male fertility in humans is currently unknown. The reversibility of these potential 
effects is unknown. The potential risk of reduced fertility or infertility should be discussed with male 
patients before initiating treatment. 
 
Haematological abnormalities 
 
ANC < 1 × 109 cells/L (see section 4.8) and ALC < 0.5 × 109 cells/L were reported in ≤ 1% of patients 
in clinical studies. Treatment should not be initiated, or should be temporarily interrupted, in patients 
with an ANC < 1 × 109 cells/L, ALC < 0.5 × 109 cells/L or haemoglobin < 8 g/dL observed during 
routine patient management (see section 4.2). 
 
Vaccinations 
 
Use of live vaccines during, or immediately prior to, filgotinib treatment is not recommended. It is 
recommended that immunisations be updated in agreement with current immunisation guidelines prior 
to initiating filgotinib treatment. 
 



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Lipids 
 
Treatment with filgotinib was associated with dose-dependent increases in lipid parameters, including 
total cholesterol, and high-density lipoprotein (HDL) levels, while low-density lipoprotein (LDL) 
levels were slightly increased (see section 4.8). LDL cholesterol returned to pre-treatment levels in the 
majority of patients who started statin therapy while taking filgotinib. The effect of these lipid 
parameter elevations on cardiovascular morbidity and mortality has not been determined (see 
section 4.2 for monitoring guidance). 
 
Cardiovascular risk 
 
Rheumatoid arthritis patients have an increased risk for cardiovascular disorders. Patients should have 
risk factors (e.g., hypertension, hyperlipidaemia) managed as part of usual standard of care. 
 
Venous thromboembolism 
 
Events of deep venous thrombosis (DVT) and pulmonary embolism (PE) have been reported in 
patients receiving JAK inhibitors including filgotinib. JAK inhibitors should be used with caution in 
patients with risk factors for DVT/PE, such as older age, obesity, a medical history of DVT/PE, or 
patients undergoing surgery, and prolonged immobilisation. If clinical features of DVT/PE occur, 
filgotinib treatment should be discontinued and patients should be evaluated promptly, followed by 
appropriate treatment. 
 
Lactose content 
 
Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or 
glucose-galactose malabsorption should not take this medicinal product. 
 
4.5 Interaction with other medicinal products and other forms of interaction 
 
Effect of other medicinal products on filgotinib 
 
Filgotinib is primarily metabolised by carboxylesterase 2 (CES2), which can be inhibited in vitro by 
medicinal products such as fenofibrate, carvedilol, diltiazem or simvastatin. The clinical relevance of 
this interaction is unknown. 
 
Effect of filgotinib on other medicinal products 
 
Filgotinib is not a clinically relevant inhibitor or inducer of most enzymes or transporters commonly 
involved in interactions such as cytochrome P450 (CYP) enzymes and UDP-glucuronosyltransferases 
(UGT). 
 
In vitro studies are inconclusive regarding the potential of filgotinib to induce CYP2B6. In vivo 
induction cannot be excluded. 
 
In vitro studies are inconclusive regarding the potential of filgotinib to induce or inhibit CYP1A2. No 
clinical studies have been performed to investigate interactions with CYP1A2 substrates and therefore 
the potential in vivo effect of concomitant induction and inhibition of CYP1A2 by filgotinib is 
unknown. Caution is recommended when filgotinib is co-administered with CYP1A2 substrates with a 
narrow therapeutic index. 
 
In vitro studies are inconclusive regarding the potential of the primary metabolite of filgotinib, 
GS-829845 to inhibit P-gp or BCRP. In vivo inhibition of these transporters cannot be excluded, and 
caution is recommended when substrates with a narrow therapeutic index (e.g., digoxin) are 
co-administered with filgotinib. 
 



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In vitro studies indicate that filgotinib and its primary metabolite GS-829845 are inhibitors of 
OATP1B1 and OATP1B3. No clinical studies have been performed to investigate interactions with 
OATP1B1 and OATP1B3 substrates. Therefore, it cannot be excluded that co-administration of 
filgotinib with OATP1B1 or OATP1B3 substrates may increase their exposure and the risk of adverse 
events. Co-administration with sensitive OATP1B1 or OATP1B3 substrates (e.g., valsartan, statins) is 
therefore not recommended. 
 
In a clinical pharmacology study, there was no effect on the pharmacokinetics of the combined 
contraceptive ethinyl estradiol and levonorgestrel when co-administered with filgotinib; thus no dose 
adjustment of oral contraceptives is required. 
 
4.6 Fertility, pregnancy and lactation 
 
Women of childbearing potential / Contraception 
 
Women of childbearing potential have to use effective contraception during and for at least 1 week 
after cessation of filgotinib treatment. 
 
Pregnancy 
 
There are no or limited amount of data from the use of filgotinib in pregnant women. Studies in 
animals have shown reproductive toxicity (see section 5.3). 
 
Based on findings in animals, filgotinib may cause foetal harm and is therefore contraindicated during 
pregnancy (see section 4.3). 
 
Breast-feeding 
 
It is unknown whether filgotinib is excreted in human milk. A risk to breastfed newborns/infants 
cannot be excluded. Therefore, Jyseleca should not be used during breast-feeding. 
 
Fertility 
 
In animal studies, decreased fertility, impaired spermatogenesis, and histopathological effects on male 
reproductive organs were observed (see section 5.3). The potential effect of filgotinib on sperm 
production and male fertility in humans is currently unknown. The reversibility of these potential 
effects is unknown (see section 4.4). 
 
Animal studies did not indicate effects with respect to fertility in females. 
 
4.7 Effects on ability to drive and use machines 
 
Filgotinib has no or negligible influence on the ability to drive and use machines. However, patients 
should be advised that dizziness has been reported during treatment with Jyseleca (see section 4.8). 
 
4.8 Undesirable effects 
 
Summary of the safety profile 
 
The most frequently reported adverse reactions are nausea (3.5%), upper respiratory tract infection 
(URTI, 3.3%), urinary tract infection (UTI, 1.7%) and dizziness (1.2%). 
 
Tabulated list of adverse reactions 
 
The following adverse reactions are based on clinical studies (Table 2). The adverse reactions are 
listed below by system organ class and frequency. Frequencies are defined as follows: common 
(≥ 1/100 to < 1/10) and uncommon (≥ 1/1,000 to < 1/100). 



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Table 2: Adverse reactions 
 

Frequency a Adverse reaction 
Infections and infestations 
Common Urinary tract infection (UTI) 

Upper respiratory tract infection (URTI) 
Uncommon Herpes zoster 

Pneumonia 
Blood and lymphatic system disorders 
Uncommon Neutropenia 
Metabolism and nutrition disorders 
Uncommon Hypercholesterolaemia 
Nervous system disorders 
Common Dizziness 
Gastrointestinal disorders 
Common Nausea 
Investigations 
Uncommon Blood creatine phosphokinase increased 
a Frequency based on placebo-controlled pre-rescue period (week 12) pooled across FINCH 1 and 2, and 

DARWIN 1 and 2, for patients who received filgotinib 200 mg. 
 
Laboratory changes 
 
Creatinine 
An increase in serum creatinine occurred with filgotinib treatment. At week 24 in the Phase 3 studies 
(FINCH 1, 2, and 3), the mean (SD) increase from baseline in serum creatinine was 0.07 (0.12) and 
0.04 (0.11) mg/dL for filgotinib 200 mg and 100 mg, respectively. Mean creatinine values remained 
within the normal range. 
 
Lipids 
Treatment with filgotinib was associated with dose-dependent increases in total cholesterol and HDL 
levels, while LDL levels were slightly increased. LDL/HDL ratios were generally unchanged. Lipid 
changes were observed within the first 12 weeks of filgotinib treatment and remained stable thereafter. 
 
Description of selected adverse reactions 
 
Infections 
In placebo-controlled studies with background DMARDs (FINCH 1, FINCH 2, DARWIN 1, and 
DARWIN 2), the frequency of infection over 12 weeks in the filgotinib 200 mg group was 18.1% 
compared to 13.3% in the placebo group. In the MTX-controlled study FINCH 3, the frequency of 
infection over 24 weeks in the filgotinib 200 mg monotherapy and filgotinib 200 mg plus MTX groups 
was 25.2% and 23.1%, respectively, compared to 24.5% in the MTX group. The overall 
exposure-adjusted incidence rate (EAIR) of infections for the filgotinib 200 mg group across all seven 
Phase 2 and 3 clinical studies (2,267 patients) was 26.5 per 100 patient-years of exposure (PYE). 
 
In placebo-controlled studies with background DMARDs, the frequency of serious infection over 
12 weeks in the filgotinib 200 mg group was 1.0% compared to 0.6% in the placebo group. In the 
MTX-controlled study FINCH 3, the frequency of serious infection over 24 weeks in the filgotinib 
200 mg monotherapy and filgotinib 200 mg plus MTX groups was 1.4% and 1.0%, respectively, 
compared to 1.0% in the MTX group. The overall EAIR of serious infections for the filgotinib 200 mg 
group across all seven Phase 2 and 3 clinical studies (2,267 patients) was 1.7 per 100 PYE. The most 
common serious infection was pneumonia. The EAIR of serious infections remained stable with 
long-term exposure. 
 



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There was a higher incidence of serious infections in patients aged 75 years and older, although data 
are limited. 
 
In placebo-controlled studies with background DMARDs, the frequencies of infectious ADRs over 
12 weeks for filgotinib 200 mg compared to placebo were: URTI (3.3% versus 1.8%), UTI (1.7% 
versus 0.9%), pneumonia (0.6% versus 0.4%), and herpes zoster (0.1% versus 0.3%). Most of the 
herpes zoster events involved a single dermatome and were non-serious. 
 
Opportunistic infections (excluding TB) 
In placebo-controlled studies with background DMARDs, there were no opportunistic infections over 
12 weeks in the filgotinib 200 mg group or the placebo group. In the MTX-controlled study FINCH 3, 
the frequency of opportunistic infections over 24 weeks was 0, 0.2%, and 0 in the filgotinib 200 mg 
monotherapy, filgotinib 200 mg plus MTX, and MTX groups, respectively. The overall EAIR of 
opportunistic infections for the filgotinib 200 mg group across all seven Phase 2 and 3 clinical studies 
(2,267 patients) was 0.1 per 100 PYE. 
 
Nausea 
Nausea was generally transient and reported during the first 24 weeks of filgotinib treatment. 
 
Creatine phosphokinase 
Dose-dependent increases in creatine phosphokinase (CPK) occurred within the first 12 weeks of 
filgotinib treatment and remained stable thereafter. At week 24 in the Phase 3 studies (FINCH 1, 2, 
and 3), the mean (SD) increase from baseline in CPK was -16 (449), 61 (260), and 33 (80) U/L for 
placebo, filgotinib 200 mg and 100 mg, respectively. 
 
In placebo-controlled Phase 3 studies with background DMARDs (FINCH 1 and FINCH 2) through 
12 weeks, CPK elevations > 5 × upper limit of normal (ULN) were reported in 0.5%, 0.3%, and 0.3% 
of patients in the placebo, filgotinib 200 mg, and filgotinib 100 mg groups, respectively. Most 
elevations > 5 × ULN did not require treatment discontinuation. 
 
Experience from long-term extension studies 
 
In the long-term extension study DARWIN 3, among patients enrolled from DARWIN 1 (N = 497), 
238 patients received filgotinib 200 mg once a day for a median duration of 4.4 years; among patients 
enrolled from DARWIN 2 (N = 242), 234 patients received filgotinib 200 mg once a day for a median 
duration of 4.4 years. The safety profile of filgotinib was similar to that in the Phase 2 and Phase 3 
studies. 
 
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 
 
Filgotinib has been administered in clinical studies following single and once daily administration up 
to 450 mg without dose-limiting toxicity. Adverse reactions were comparable to those seen at lower 
doses and no specific toxicities were identified. Pharmacokinetic data following a single dose of 
100 mg filgotinib in healthy subjects indicate that approximately 50% of the administered dose is 
eliminated within 24 hours of dosing and 90% of the dose is eliminated within 72 hours. In case of an 
overdose, it is recommended that a patient be monitored for signs and symptoms of adverse reactions. 
Treatment of overdose with filgotinib consists of general supportive measures including monitoring of 
vital signs as well as observation of the clinical status of the patient. It is unknown whether filgotinib 
can be removed by dialysis. 
 

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


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5. PHARMACOLOGICAL PROPERTIES 
 
5.1 Pharmacodynamic properties 
 
Pharmacotherapeutic group: Immunosuppressants, selective immunosuppressants, ATC code: 
L04AA45 
 
Mechanism of action 
 
Filgotinib is an adenosine triphosphate (ATP)-competitive and reversible inhibitor of the JAK family. 
JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor 
interactions on the cellular membrane. JAK1 is important in mediating inflammatory cytokine signals, 
JAK2 in mediating myelopoiesis and erythropoiesis and JAK3 plays critical roles in immune 
homeostasis and lymphopoiesis. Within the signalling pathway, JAKs phosphorylate and activate 
signal transducers and activators of transcription (STATs) which modulate intracellular activity 
including gene expression. Filgotinib modulates these signalling pathways by preventing the 
phosphorylation and activation of STATs. In biochemical assays, filgotinib preferentially inhibited the 
activity of JAK1 and showed > 5-fold higher potency of filgotinib for JAK1 over JAK2, JAK3 and 
TYK2. In human cellular assays, filgotinib preferentially inhibited JAK1/JAK3-mediated signalling 
downstream of the heterodimeric cytokine receptors for interleukin (IL)-2, IL-4 and IL-15, 
JAK1/2-mediated IL-6, and JAK1/TYK2-mediated type I interferons, with functional selectivity over 
cytokine receptors that signal via pairs of JAK2 or JAK2/TYK2. GS-829845, the primary metabolite 
of filgotinib, was approximately 10-fold less active than filgotinib in in vitro assays, while exhibiting a 
similar JAK1 preferential inhibitory activity. In an in vivo rat model, the overall pharmacodynamic 
effect was predominantly driven by the metabolite. 
 
Pharmacodynamic effects 
 
Inhibition of IL-6 induced STAT1 phosphorylation 
Filgotinib administration resulted in a dose-dependent inhibition of IL-6 induced STAT1 
phosphorylation in whole blood from healthy subjects. Filgotinib administration did not affect 
JAK2-associated GM-CSF induced STAT5 phosphorylation. 
 
Immunoglobulins 
In FINCH 1, 2, and 3, the median and interquartile ranges for serum IgG, IgM, and IgA values 
remained largely within the normal reference ranges through 24 weeks of treatment with filgotinib. 
 
Haematologic effects 
Treatment with filgotinib was associated with a small, transient increase in mean ALC that remained 
within normal reference ranges and gradually returned to at or near baseline levels with continued 
treatment by week 12. In FINCH 1, 2, and 3, median haemoglobin values remained stable within the 
normal range through 24 weeks of filgotinib treatment. A slight decrease in median platelet counts 
occurred within the first 4 weeks of filgotinib treatment and remained stable thereafter through 
24 weeks. Median platelet counts remained within the normal range. 
 
C-reactive protein 
Decreases in serum C-reactive protein (CRP) were observed as early as 2 weeks after starting 
treatment with filgotinib and were maintained through 24 weeks of treatment. 
 
Clinical efficacy and safety 
 
The efficacy and safety of filgotinib once daily were assessed in three Phase 3 studies (FINCH 1, 2, 
and 3). These were randomised, double-blind, multicentre studies in patients with moderate to severe 
active rheumatoid arthritis diagnosed according to American College of Rheumatology 
(ACR)/European League Against Rheumatism (EULAR) 2010 criteria. 
 



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FINCH 1 was a 52-week study in 1,755 patients with rheumatoid arthritis who had an inadequate 
response to MTX. Patients received filgotinib 200 mg once daily, filgotinib 100 mg once daily, 
adalimumab every 2 weeks, or placebo, all added to stable background MTX. At week 24, patients 
receiving placebo were re-randomised to filgotinib 100 mg or 200 mg once daily through week 52. 
The primary endpoint was the proportion of patients who achieved an ACR20 response at week 12. 
 
FINCH 2 was a 24-week study in 448 patients with rheumatoid arthritis who had an inadequate 
response to bDMARDs. Patients received filgotinib 200 mg once daily, filgotinib 100 mg once daily, 
or placebo, all with a continued stable background dose of conventional synthetic DMARD(s) 
(csDMARD[s]: MTX, hydroxychloroquine, sulfasalazine, or leflunomide). The primary endpoint was 
the proportion of patients who achieved an ACR20 response at week 12. 
 
FINCH 3 was a 52-week study in 1,249 patients with rheumatoid arthritis who were naïve to MTX 
therapy. Patients received filgotinib 200 mg once daily plus MTX once weekly, filgotinib 100 mg once 
daily plus MTX once weekly, filgotinib 200 mg (monotherapy) once daily, or MTX (monotherapy) 
once weekly. The primary endpoint was the proportion of patients who achieved an ACR20 response 
at week 24. 
 
Clinical response 
Higher response rates versus placebo or MTX were seen at week 2 for ACR20, and responses were 
maintained through week 52. 
 
Treatment with filgotinib 200 mg resulted in improvements in all individual ACR components, 
including tender and swollen joint counts, patient and physician global assessments, Health 
Assessment Questionnaire Disability Index (HAQ-DI), pain assessment and high sensitivity CRP, 
compared to placebo or MTX. In two of the Phase 3 studies (FINCH 1 and FINCH 2), the comparison 
(versus placebo) was carried out on top of MTX or csDMARD(s) (see above). 
 
Low disease activity and remission 
Across the Phase 3 studies, a significantly higher proportion of patients treated with filgotinib 200 mg 
plus MTX or other csDMARD achieved low disease activity and/or remission (DAS28-CRP ≤ 3.2 and 
DAS28-CRP < 2.6) at weeks 12 and 24 as compared to placebo or MTX. Filgotinib 200 mg was 
non-inferior to adalimumab at week 12 for DAS28-CRP ≤ 3.2 in FINCH 1 (Table 3). 
 
Table 3: Clinical response at weeks 12, 24 and 52 in FINCH 1, 2, and 3 
 

 FINCH 1 MTX-IR 
FINCH 2 

bDMARD-IR 
FINCH 3 

MTX-naïve 

Treatment 
FIL 

200 mg 
FIL 

100 mg ADA PBO 
FIL 

200 mg 
FIL 

100 mg PBO 
FIL 

200 mg 
+ MTX 

FIL 
100 mg 
+ MTX 

FIL 
200 mg 
mono 

MTX 
+ MTX + csDMARD 

N 475 480 325 475 147 153 148 416 207 210 416 
Week 
ACR20 (percent of patients) 

12 77***¶ 70*** 71 50 66*** 58*** 31 77††† 72†† 71†† 59 
24 78††† 78††† 74 59 69††† 55††† 34 81*** 80* 78 71 
52 78 76 74 - - - - 75††† 73†† 75††† 62 

ACR50 (percent of patients) 
12 47†††¶¶¶ 36††† 35 20 43††† 32††† 15 53††† 44††† 46††† 28 
24 58††† 53††† 52 33 46††† 35†† 19 62††† 57†† 58†† 46 
52 62 59 59 - - - - 62††† 59†† 61††† 48 

ACR70 (percent of patients) 
12 26†††¶¶¶ 19††† 14 7 22††† 14† 7 33††† 27††† 29††† 13 
24 36†††¶ 30††† 30 15 32††† 20†† 8 44††† 40††† 40††† 26 
52 44 38 39 - - - - 48††† 40†† 45††† 30 



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 FINCH 1 MTX-IR 
FINCH 2 

bDMARD-IR 
FINCH 3 

MTX-naïve 

Treatment 
FIL 

200 mg 
FIL 

100 mg ADA PBO 
FIL 

200 mg 
FIL 

100 mg PBO 
FIL 

200 mg 
+ MTX 

FIL 
100 mg 
+ MTX 

FIL 
200 mg 
mono 

MTX 
+ MTX + csDMARD 

N 475 480 325 475 147 153 148 416 207 210 416 
DAS28-CRP ≤ 3.2 (percent of patients) 

12 50***### 39*** 43 23 41*** 37*** 16 56††† 50††† 48††† 29 
24 61†††§§§¶¶ 53†††§§§ 50 34 48††† 38††† 21 69††† 63††† 60††† 46 
52 66¶ 59 59 - - - - 69††† 60†† 66††† 48 

DAS28-CRP < 2.6 (percent of patients) 
12 34†††§§§¶¶¶ 24†††§§ 24 9 22††† 25††† 8 40††† 32††† 30††† 17 
24 48***§§§¶¶¶ 35***§§§ 36 16 31††† 26†† 12 54*** 43*** 42††† 29 
52 54¶ 43 46 - - - - 53††† 43†† 46††† 31 

CDAI, change from baseline (mean) 
12 -26.0††† -23.3††† -23.5 -20.3 -26.2††† -23.8††† -17.3 -27.8††† -26.1††† -27.5††† -22.7 
24 -30.6††† -28.6††† -28.4 -26.3 -30.9††† -27.8†† -25.4 -31.3††† -30.0††† -31.3††† -28.2 
52 -32.9 -30.9 -31.6 - - - - -33.8††† -31.9† -33.6††† -31.2 

ADA: adalimumab; bDMARD: biologic DMARD; csDMARD: conventional synthetic DMARD; DMARD: 
disease-modifying antirheumatic drug; FIL: filgotinib; IR: inadequate responder; mono: monotherapy; MTX: methotrexate; 
PBO: placebo. 
* p ≤ 0.05; ** p ≤ 0.01; *** p ≤ 0.001 versus placebo (versus MTX for FINCH 3) (statistically significant difference with 

multiplicity adjustment). 
† p ≤ 0.05; †† p ≤ 0.01; ††† p ≤ 0.001 versus placebo (versus MTX for FINCH 3) (nominal p-value). 
# p ≤ 0.05; ## p ≤ 0.01; ### p ≤ 0.001 versus adalimumab for FINCH 1 (non-inferiority test, statistically significant 

difference with multiplicity adjustment) (analysed for DAS28-CRP ≤ 3.2 and < 2.6 pairwise comparisons only). 
§ p ≤ 0.05; §§ p ≤ 0.01; §§§ p ≤ 0.001 versus adalimumab for FINCH 1 (non-inferiority test, nominal p-value) (analysed 

for DAS28-CRP ≤ 3.2 and < 2.6 pairwise comparisons only). 
¶ p ≤ 0.05; ¶¶ p ≤ 0.01; ¶¶¶ p ≤ 0.001 versus adalimumab for FINCH 1 (superiority test, nominal p-value) (analysed for 

ACR20/50/70, and DAS28-CRP ≤ 3.2 and < 2.6 pairwise comparisons only). 
Note: Comparisons were carried out on top of a stable background of MTX (FINCH 1) or csDMARD(s) (FINCH 2). 
 
Radiographic response 
Inhibition of progression of structural joint damage was assessed using the modified Total Sharp Score 
(mTSS) and its components, the erosion score and joint space narrowing score, at weeks 24 and 52 in 
FINCH 1 and FINCH 3. 
 
In patients who had an inadequate response to MTX, treatment with filgotinib plus MTX resulted in 
statistically significant inhibition of progression of structural joint damage compared to placebo plus 
MTX at week 24 (Table 4). Analyses of erosion and joint space narrowing scores were consistent with 
the overall scores. 
 



13 

Table 4: Radiographic response at weeks 24 and 52 in FINCH 1 and 3 
 

 FINCH 1 MTX-IR 
FINCH 3 

MTX-naïve 

Treatment 
FIL 

200 mg 
FIL 

100 mg ADA PBO 
FIL 

200 mg 
+ MTX 

FIL 
100 mg 
+ MTX 

FIL 
200 mg 
mono 

MTX 
+ MTX 

N 475 480 325 475 416 207 210 416 
Week 
Modified Total Sharp Score (mTSS), mean (SD) change from baseline 

24 0.13 
(0.94)*** 

0.17 
(0.91)*** 

0.16 
(0.95) 

0.37 
(1.42) 

0.21 
(1.68) 

0.22 
(1.53) 

-0.04 
(1.71)†† 

0.51 
(2.89) 

52 0.21 
(1.43) 

0.50 
(2.10) 

0.58 
(3.62) - 

0.31 
(1.81)††† 

0.23 
(1.11)†† 

0.33 
(1.90)†† 

0.81 
(3.09) 

Proportion of patients with no radiographic progression a 
24 88%** 86% 86% 81% 81%† 77% 83%† 72% 
52 88% 81% 82% - 81%†† 76% 77% 71% 

ADA: adalimumab; FIL: filgotinib; IR: inadequate responder; mono: monotherapy; MTX: methotrexate; PBO: placebo. 
a No progression defined as mTSS change ≤ 0. 
* p ≤ 0.05; ** p ≤ 0.01; *** p ≤ 0.001 versus placebo (statistically significant difference with multiplicity adjustment). 
† p ≤ 0.05; †† p ≤ 0.01; ††† p ≤ 0.001 versus placebo (versus MTX for FINCH 3) (nominal p-value). 
 
Physical function response and health related outcomes 
Treatment with filgotinib 200 mg resulted in a significant improvement in physical function, as 
measured by change from baseline in HAQ-DI (Table 5). 
 
Table 5: Mean change from baseline in HAQ-DI at weeks 12, 24 and 52 in FINCH 1, 2, and 3 
 

 
Mean change from baseline 

FINCH 1 
MTX-IR 

FINCH 2 
bDMARD-IR 

FINCH 3 
MTX-naïve 

Treatment 
FIL 

200 mg 
FIL 

100 mg ADA PBO 
FIL 

200 mg 
FIL 

100 mg PBO 
FIL 

200 mg 
+ MTX 

FIL 
100 mg 
+ MTX 

FIL 
200 mg 
mono 

MTX 
+ MTX + csDMARD 

N 475 480 325 475 147 153 148 416 207 210 416 
Week 
Health Assessment Questionnaire Disability Index (HAQ-DI) 
Baseline 

score 1.59 1.55 1.59 1.63 1.70 1.64 1.65 1.52 1.56 1.56 1.60 

12 -0.69*** -0.56*** -0.61 -0.42 -0.55*** -0.48*** -0.23 -0.85††† -0.77††† -0.76††† -0.61 
24 -0.82††† -0.75††† -0.78 -0.62 -0.75††† -0.60†† -0.42 -0.94*** -0.90** -0.89† -0.79 
52 -0.93 -0.85 -0.85 - - - - -1.00††† -0.97 -0.95† -0.88 

ADA: adalimumab; bDMARD: biologic DMARD; csDMARD: conventional synthetic DMARD; DMARD: 
disease-modifying antirheumatic drug; FIL: filgotinib; IR: inadequate responder; mono: monotherapy; MTX: methotrexate; 
PBO: placebo. 
* p ≤ 0.05; ** p ≤ 0.01; *** p ≤ 0.001 versus placebo (statistically significant difference with multiplicity adjustment). 
† p ≤ 0.05; †† p ≤ 0.01; ††† p ≤ 0.001 versus placebo (versus MTX for FINCH 3) (nominal p-value). 
 
Health status outcomes were assessed by the Short Form health survey (SF-36). Patients treated with 
filgotinib 200 mg plus MTX or other csDMARD demonstrated numerically greater improvement from 
baseline in the physical component summary score of SF-36 as well as in the Functional Assessment 
of Chronic Illness Therapy-Fatigue score (FACIT-F) at weeks 12 and 24 compared to placebo plus 
MTX/csDMARD or MTX. 
 
Long-term efficacy 
In a long-term Phase 2 open-label extension study (DARWIN 3), continued and durable responses 
were observed, with ACR20/50/70 responses maintained for up to 3 years in patients who received 
filgotinib 200 mg as monotherapy or with MTX. 
 



14 

Paediatric population 
 
The European Medicines Agency has deferred the obligation to submit the results of studies with 
filgotinib in one or more subsets of the paediatric population in the treatment of chronic idiopathic 
arthritis (including rheumatoid arthritis, ankylosing spondylarthritis, psoriatic arthritis, and juvenile 
idiopathic arthritis) (see section 4.2 for information on paediatric use). 
 
5.2 Pharmacokinetic properties 
 
Absorption 
 
Following oral administration, filgotinib was absorbed quickly and its median peak plasma 
concentration was observed 2 to 3 hours postdose after multiple dosing; the median peak plasma 
concentrations of its primary metabolite GS-829845 were observed 5 hours postdose after multiple 
dosing. Filgotinib and GS-829845 exposures (AUC) and Cmax were similar in healthy adult subjects 
and patients with rheumatoid arthritis. Filgotinib and GS-829845 exposures (AUC) and Cmax are 
dose-proportional over the therapeutic dose range. Steady-state concentrations of filgotinib are 
achieved in 2 - 3 days with negligible accumulation after once daily administration. Steady-state 
concentrations of GS-829845 are achieved in 4 days with approximately 2-fold accumulation after 
once daily dosing of filgotinib. 
 
There were no clinically relevant differences in exposures when filgotinib was administered with a 
high-fat or low-fat meal as compared to a fasted state. Filgotinib can be administered with or without 
food. 
 
The multiple dose pharmacokinetic parameters of filgotinib and GS-829845 are provided in Table 6. 
 
Table 6: Multiple dose pharmacokinetic parameters of filgotinib and GS-829845 following oral 
administration of filgotinib 200 mg with or without food in adults with moderate to severe active 
rheumatoid arthritis 
 

Parameter a 
Mean (%CV) Filgotinib 

b GS-829845 c 

Cmax (µg/mL) 2.15 (48.1) 4.43 (29.3) 
AUCtau (µg•h/mL) 6.77 (43.7) 83.2 (27.3) 
CV: coefficient of variation. 
a From intensive PK analyses of studies FINCH 1, FINCH 2, and FINCH 3 in rheumatoid arthritis patients receiving 

200 mg filgotinib once daily. 
b N = 37 
c N = 33 
 
Distribution 
 
Filgotinib and GS-829845 binding to human plasma proteins is low (55 - 59% and 39 - 44% bound, 
respectively). The blood-to-plasma ratio of filgotinib ranged from 0.85 to 1.1 indicating no preferential 
distribution of filgotinib and GS-829845 into blood cells. Filgotinib and GS-829845 are substrates of 
the P-gp transporter. 
 
Biotransformation 
 
Filgotinib is extensively metabolised with approximately 9.4% and 4.5% of an orally administered 
dose recovered as unchanged filgotinib in urine and faeces, respectively. Filgotinib is primarily 
metabolised by CES2, and to a lesser extent by CES1. Both CES2 and CES1 form GS-829845, an 
active circulating metabolite that is approximately 10-fold less potent than the parent compound. In a 
clinical pharmacology study, filgotinib and GS-829845 accounted for the majority of radioactivity 
circulating in plasma (2.9% and 92%, respectively). No other major metabolites were identified. 
 



15 

As both filgotinib and GS-829845 contribute to efficacy, their exposures were combined into a single 
parameter, AUCeff. AUCeff is the sum of the AUC of filgotinib and GS-829845, corrected for their 
respective molecular weights and potencies. 
 
Elimination 
 
Approximately 87% of the administered dose was eliminated in the urine as filgotinib and its 
metabolites, while about 15% of the dose was eliminated in the faeces. GS-829845 accounted for 
approximately 54% and 8.9% of dose recovered in urine and faeces, respectively. The mean terminal 
half-lives of filgotinib and GS-829845 were approximately 7 and 19 hours, respectively. 
 
Other special populations 
 
Weight, gender, race, and age 
Bodyweight, gender, race, and age did not have a clinically relevant effect on the pharmacokinetics 
(AUC) of filgotinib or GS-829845. 
 
Elderly 
There were no clinically relevant differences in mean filgotinib and GS-829845 exposures (AUC and 
Cmax) between older patients aged ≥ 65 years relative to adult patients aged < 65 years. 
 
Renal impairment 
The pharmacokinetics of filgotinib and GS-829845 were unaffected in subjects with mild renal 
impairment (CrCl 60 to < 90 mL/min). Increases in exposures (AUC) of filgotinib, GS-829845, and 
combined AUCeff (≤ 2-fold), were observed in subjects with moderate renal impairment (CrCl 30 to 
< 60 mL/min). In subjects with severe renal impairment (CrCl 15 to < 30 mL/min), filgotinib exposure 
(AUC) increased by 2.2-fold and GS-829845 exposure significantly increased by 3.5-fold leading to a 
3-fold increase in AUCeff. The pharmacokinetics of filgotinib has not been studied in subjects with end 
stage renal disease (CrCl < 15 mL/min). 
 
Hepatic impairment 
No clinically relevant changes in the exposures (AUC) of filgotinib and GS-829845 individually, or 
their combined exposure (AUCeff), were observed in subjects with moderate hepatic impairment 
(Child-Pugh B). The pharmacokinetics of filgotinib has not been studied in subjects with severe 
hepatic impairment (Child-Pugh C). 
 
Effect of filgotinib on other medicinal products 
 
Potential interactions between filgotinib and co-administered medicinal products are listed in Table 7 
below (increase is indicated as “↑”, decrease as “↓”, and no change as “↔”; no effect boundaries are 
70 - 143% unless otherwise indicated). 
 
Table 7: Interaction studies with filgotinib 1 
 
Medicinal product by therapeutic 

areas/Possible mechanism of 
interaction 

Effects on medicinal product levels. 
Mean percent change in AUC, Cmax 

Recommendation concerning 
co-administration with 

filgotinib 
ANTI-INFECTIVES 
Antimycobacterials 
Rifampicin (600 mg once daily) 2 
 
(P-gp induction) 

Filgotinib: 
AUC: ↓ 27% 
Cmax: ↓ 26% 
 
GS-829845: 
AUC: ↓ 38% 
Cmax: ↓ 19% 
 
AUCeff 6: ↓ 33% 

No dose adjustment is required 
upon co-administration. 



16 

Medicinal product by therapeutic 
areas/Possible mechanism of 

interaction 

Effects on medicinal product levels. 
Mean percent change in AUC, Cmax 

Recommendation concerning 
co-administration with 

filgotinib 
Antifungals 
Itraconazole (200 mg single dose) 3 
 
(P-gp inhibition) 

Filgotinib: 
AUC: ↑ 45% 
Cmax: ↑ 64% 
 
GS-829845: 
AUC: ↔ 
Cmax: ↔ 
 
AUCeff: ↑ 21% 

No dose adjustment is required 
upon co-administration. 

GASTRIC ACID REDUCING AGENTS 
Famotidine (40 mg twice daily) 2 
 
(Increases gastric pH) 

Filgotinib: 
AUC: ↔ 
Cmax: ↔ 
 
GS-829845: 
AUC: ↔ 
Cmax: ↔ 

No dose adjustment is required 
upon co-administration. 

Omeprazole (40 mg once daily) 2 
 
(Increases gastric pH) 

Filgotinib: 
AUC: ↔ 
Cmax: ↓ 27% 
 
GS-829845: 
AUC: ↔ 
Cmax: ↔ 

No dose adjustment is required 
upon co-administration. 

ORAL ANTI-DIABETICS 
Metformin (850 mg single dose) 4 
 
(Inhibition of OCT2, MATE1, and 
MATE-2K) 

Metformin: 
AUC: ↔ 
Cmax: ↔ 

No dose adjustment is required 
upon co-administration. 

ORAL CONTRACEPTIVES 
Ethinyl estradiol (0.03 mg single 
dose)/Levonorgestrel (0.15 mg 
single dose) 4 

Ethinyl estradiol: 
AUC: ↔ 
Cmax: ↔ 
 
Levonorgestrel: 
AUC: ↔ 
Cmax: ↔ 

No dose adjustment is required 
upon co-administration. 

SEDATIVES/HYPNOTICS 
Midazolam (2 mg single dose) 4,5 
 
(Inhibition of CYP3A4) 

Midazolam: 
AUC: ↔ 
Cmax: ↔ 
 
1’OH-midazolam: 
AUC: ↔ 
Cmax: ↔ 

No dose adjustment is required 
upon co-administration. 

GS-829845: primary metabolite of filgotinib. 
1 All interaction studies conducted in healthy volunteers. 
2 Study conducted with filgotinib 200 mg single dose. 
3 Study conducted with filgotinib 100 mg single dose. 
4 Study conducted with filgotinib 200 mg once daily. 
5 Bioequivalence boundaries are 80 - 125% for midazolam and 1’OH-midazolam. 
6 As both filgotinib and GS-829845 contribute to efficacy, their exposures were combined into a single parameter, AUCeff. 

AUCeff is the combined AUC of filgotinib and GS-829845, adjusted for their respective molecular weights and potencies. 
 
Potential for filgotinib to affect other medicinal products 
In vitro data indicate that filgotinib and GS-829845 do not inhibit the activity of the following: 
CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, UGT1A1, UGT1A4, UGT1A6, UGT1A9, and 



17 

UGT2B7 at clinically relevant concentrations. The potential for filgotinib to induce CYP2B6 
constitutive androstane receptor (CAR) mediated metabolism in vivo is unknown. No conclusion can 
be drawn from the in vitro data regarding the potential of filgotinib to inhibit or induce CYP1A2. 
In vivo data demonstrated no inhibition or induction of CYP3A4 mediated metabolism. 
 
In vitro studies indicate that filgotinib and GS-829845 are not inhibitors of OCT1, BSEP, OAT1, 
OAT3 or OAT4 at clinically relevant concentrations. In vitro data indicate that filgotinib and 
GS-829845 have the potential to inhibit OATP1B1, OATP1B3, OCT2, MATE1 (filgotinib only), and 
MATE-2K. While in vitro studies indicate that filgotinib is not an inhibitor of P-gp or BCRP, the 
results for GS-829845 are inconclusive and in vivo inhibition of P-gp or BCRP by GS-829845 cannot 
be excluded. 
 
5.3 Preclinical safety data 
 
Non-clinical data reveal no special hazard for humans based on conventional studies of safety 
pharmacology. 
 
The carcinogenic potential of filgotinib was evaluated in a 6-month rasH2 transgenic mouse study and 
a 2-year rat study. Filgotinib was not carcinogenic in mice at up to 150 mg/kg/day, which resulted in 
exposures of approximately 25 and 12 times the exposures in humans at the 100 mg and 200 mg once 
daily doses, respectively. In the 2-year rat study, filgotinib treatment resulted in an increase in 
incidence and decrease in latency of benign Leydig cell tumours at the highest dose of 45 mg/kg/day 
(exposures of approximately 4.2 times exposures in humans at the 200 mg once daily dose); the 
clinical relevance of this finding is low. 
 
Filgotinib was not mutagenic or clastogenic in the in vitro bacterial reverse mutation assay, in vitro 
chromosome aberration assay, and in vivo rat micronucleus assay. 
 
Adverse findings of degeneration/necrosis of incisor ameloblasts were observed in rats at exposures 
21- to 28-fold greater than clinical exposures at the 200 mg filgotinib dose, with exposure margins at 
the NOAEL ranging from 3.5- to 8-fold. The human relevance of these dental findings is considered 
low since in contrast to adult patients, ameloblasts in rats persist into adulthood to support lifelong 
continuous incisor growth. 
 
Impaired spermatogenesis and histopathological effects on male reproductive organs (testes and 
epididymis) were observed with filgotinib in rats and dogs. At the no-observed-adverse-effect-levels 
(NOAELs) in dogs (the most sensitive species), the exposure margin is 2.7-fold at the 200 mg once 
daily dose in humans. The severity of the histological effects was dose-dependent. Spermatogenic and 
histopathological effects were not fully reversible at lower exposures and were irreversible at exposure 
margins of approximately 7- to 9-fold the exposure at the 200 mg once daily dose in humans. 
 
Embryo-foetal development studies in rats and rabbits demonstrated embryolethality and 
teratogenicity at exposures comparable to 200 mg filgotinib once daily dosing in humans. Visceral and 
skeletal malformations and/or variations were observed at all dose levels of filgotinib. 
 
Filgotinib was administered to pregnant rats at doses of 25, 50, and 100 mg/kg/day. Dose-related 
increases in the incidence of internal hydrocephaly, dilated ureters, and multiple vertebral anomalies 
were seen at all dose levels. At 100 mg/kg/day, an increased number of early and late resorptions were 
noted together with a decreased number of viable foetuses. In addition, foetal body weights were 
decreased. 
 
In rabbits, filgotinib caused visceral malformations mainly in the lungs and cardiovascular system, at a 
dose level of 60 mg/kg/day. Filgotinib caused skeletal malformations affecting the vertebral column 
region at dose levels of 25 and 60 mg/kg/day, mainly in vertebra, ribs and sternebrae. Fused sternebrae 
also occurred at 10 mg/kg/day filgotinib. Retarded skeletal ossification was evidenced at 60 mg/kg/day. 
 



18 

No adverse effects on pre-/postnatal development were observed in rats in a pre- and postnatal 
development study of filgotinib and GS-829845. Filgotinib and GS-829845 were detected in nursing 
rat pups after administration of filgotinib to lactating female rats from gestation day 6 through 10 days 
post-partum at dose levels of 2, 5, and 15 mg/kg/day, likely due to the presence of filgotinib in milk. 
At the highest tested dose, maternal systemic exposure (AUC) to filgotinib in rats was approximately 
2 times the exposure in humans at the 200 mg once daily dose; exposures in nursing pups were less 
than 6% that of maternal exposure on day 10 post-partum. Due to the low exposure of the animals, the 
pre-/postnatal development study was considered inconclusive. 
 
 
6. PHARMACEUTICAL PARTICULARS 
 
6.1 List of excipients 
 
Tablet core 
 
Microcrystalline cellulose 
Lactose monohydrate 
Pregelatinised starch 
Colloidal silicon dioxide 
Fumaric acid 
Magnesium stearate 
 
Film-coating 
 
Polyvinyl alcohol 
Titanium dioxide (E171) 
Macrogol 
Talc 
Iron oxide yellow (E172) 
Iron oxide red (E172) 
 
6.2 Incompatibilities 
 
Not applicable. 
 
6.3 Shelf life 
 
2 years 
 
6.4 Special precautions for storage 
 
Store in the original package in order to protect from moisture. Keep the bottle tightly closed. 
 
6.5 Nature and contents of container 
 
White, high-density polyethylene (HDPE) bottles, enclosed with a child-resistant polypropylene (PP) 
screw cap lined with an induction-sealed aluminium foil liner. Each bottle contains either a canister or 
sachet containing silica gel desiccant and polyester coil. 
 
The following pack sizes are available: outer cartons containing 1 bottle of 30 film-coated tablets and 
outer cartons containing 90 (3 bottles of 30) film-coated tablets. 
 
Not all pack sizes may be marketed. 
 



19 

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 Ireland UC 
Carrigtohill 
County Cork, T45 DP77 
Ireland 
 
 
8. MARKETING AUTHORISATION NUMBER(S) 
 
Jyseleca 100 mg film-coated tablets 
 
EU/1/20/1480/001 
EU/1/20/1480/002 
 
Jyseleca 200 mg film-coated tablets 
 
EU/1/20/1480/003 
EU/1/20/1480/004 
 
 
9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION 
 
Date of first authorisation: DD month YYYY 
 
 
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. 

http://www.ema.europa.eu/


20 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

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 

 
 



21 

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 (PSURs) 
 
The requirements for submission of PSURs for this medicinal product are set out in the list of Union 
reference dates (EURD list) provided for under Article 107c(7) of Directive 2001/83/EC and any 
subsequent updates published on the European medicines web-portal. 
 
The marketing authorisation holder (MAH) shall submit the first PSUR for this product within 
6 months following authorisation. 
 
 
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. 

 
• Additional risk minimisation measures 
 
Prior to launch of Jyseleca in each Member State the MAH must agree about the content and format of 
the educational programme, including communication media, distribution modalities, and any other 
aspects of the programme, with the National Competent Authority. 
 
The objective of the programme is to increase awareness of healthcare professionals (HCPs) and 
patients on the risks of serious and opportunistic infections, foetal malformations (pregnancy risk), 
potential effect on male fertility, venous thromboembolisms (VTEs), and major cardiovascular events 
(MACE) and the management of these risks. 
 



22 

The MAH shall ensure that in each Member State where Jyseleca is marketed, all HCPs and 
patients/carers who are expected to prescribe, dispense or use Jyseleca have access to/are provided 
with the following educational package: 
 
The HCP educational material should contain: 
• Summary of Product Characteristics 
• Guide for healthcare professionals 
• Patient Alert Card (PAC) 
 
The Guide for healthcare professionals shall contain the following key elements: 
• General introductory language that the HCP guide contains important information to assist the 

discussion with patients when prescribing filgotinib. The guide also informs on steps which can 
be taken to reduce a patient’s risk for key safety aspects of filgotinib. 

• Language for HCPs to inform patients of the importance of the PAC 
• Risk of serious and opportunistic infections including tuberculosis (TB) and herpes zoster 

o Information on the risk of infections during filgotinib treatment 
o Details on the management of the risk of infection with suggested clinical measures, i.e., 

what contraindications should be considered prior to initiation of filgotinib, screening for 
TB, herpes zoster, viral hepatitis and steps to take in the event of an infection 

o Information on avoidance of live, attenuated vaccines immediately prior to or during 
filgotinib treatment 

o Information on appropriate instructions for patients to seek urgent medical attention 
should they develop any signs suggestive of an infection 

• Risk of embryolethality and teratogenicity 
o Information on the risk of teratogenicity with filgotinib treatment 
o Details on the steps required to minimise the risk of exposure during pregnancy for 

women of childbearing potential based on the following: filgotinib is contraindicated 
during pregnancy, women of childbearing potential must be encouraged to use effective 
contraception during treatment and for at least 1 week after stopping filgotinib treatment, 
to advise patients to notify their HCP immediately if they think they could be pregnant or 
if pregnancy is confirmed, HCPs should actively discuss with patients any current or 
future pregnancy plans 

o Language to advise patients who are breast-feeding or intend to breast-feed that filgotinib 
should not be used 

• Risk of impaired spermatogenesis, leading to possible reduction in male fertility 
o Information on the potential risk of impaired spermatogenesis with filgotinib treatment, 

based on the available data 
o Language to discuss with male patients their plans to father a child, noting the potential 

for reduction in sperm count with filgotinib treatment, and the possible impact on fertility 
• Risk of venous thromboembolism (VTE) 

o Guidance on the use of filgotinib in patients with risk factors for VTE 
o Information on the risk of VTE with filgotinib treatment 
o Details on the management of the risk of VTE with suggested clinical measures, i.e., 

discontinuation of filgotinib treatment in the event of VTE clinical features occurrence, 
periodic re-evaluation of patients’ risks for VTEs 

• Risk of major adverse cardiovascular events (MACE) 
o Guidance on the use of filgotinib in patients with risk factors for MACE 
o Information on the risk of MACE with filgotinib treatment 
o Information on the risk of an increase in lipid parameters including dose-dependent 

increases in total cholesterol, and high-density lipoprotein 
• Prescribing in the very elderly (75 years and above) 

o Information on the treatment of patients aged 75 years and above with filgotinib 
o Guidance on the dose of filgotinib to be used in patients aged 75 years and above 

• Instructions for how to access digital HCP information 
• Instructions on where to report adverse events 
 



23 

The patient information pack should contain: 
• Patient information leaflet 
• Patient Alert Card (PAC) 
 
The patient alert card shall contain the following key messages: 
• Contact details of the filgotinib prescriber 
• Language that the PAC should be carried by the patient at all times and instruction to share it 

with HCPs involved in their care (i.e., non-filgotinib prescribers, emergency room HCPs, etc.) 
• Information on the signs and symptoms of deep venous thrombosis or pulmonary embolism 

which are essential for the patient to be aware of, so that medical attention can be sought 
• Information on the signs and symptoms of serious and opportunistic infections, including herpes 

zoster, that are essential for the patient to be aware of, so that medical attention can be sought 
o Information to advise patients and their HCPs about the risk of immunisation with live 

vaccines during filgotinib treatment 
• Information on pregnancy, contraception and breast-feeding 

o Clear message that filgotinib must not be used in pregnancy 
o Guidance for patients to use effective contraception while taking filgotinib, and for at 

least 1 week after stopping filgotinib treatment 
o Advice that filgotinib should not be used while breast-feeding 
o Information on the possible effect on male fertility 

• Information about monitoring cholesterol levels during treatment. 



24 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

ANNEX III 
 

LABELLING AND PACKAGE LEAFLET 
 
 



25 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

A. LABELLING 
 
 



26 

 
PARTICULARS TO APPEAR ON THE OUTER PACKAGING 
 
CARTON LABELLING FOR 100 MG FILM-COATED TABLETS 
 
 
1. NAME OF THE MEDICINAL PRODUCT 
 
Jyseleca 100 mg film-coated tablets 
filgotinib 
 
 
2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each film-coated tablet contains 100 mg filgotinib (as maleate). 
 
 
3. LIST OF EXCIPIENTS 
 
Contains lactose. 
 
 
4. PHARMACEUTICAL FORM AND CONTENTS 
 
30 film-coated tablets 
 
90 (3 bottles of 30) film-coated tablets 
 
 
5. METHOD AND ROUTE(S) OF ADMINISTRATION 
 
Read the package leaflet before use. 
 
Oral use 
 
QR code to be included 
www.jyseleca.eu 
 
 
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 
 
Do not swallow the desiccant. 
 
 
8. EXPIRY DATE 
 
EXP 
 
 

http://www.jyseleca.eu/


27 

9. SPECIAL STORAGE CONDITIONS 
 
Store in the original package in order to protect from moisture. Keep the bottle tightly closed. 
 
 
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 Ireland UC 
Carrigtohill 
County Cork, T45 DP77 
Ireland 
 
 
12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/20/1480/001 30 film-coated tablets 
EU/1/20/1480/002 90 (3 bottles of 30) film-coated tablets 
 
 
13. BATCH NUMBER 
 
Lot 
 
 
14. GENERAL CLASSIFICATION FOR SUPPLY 
 
 
15. INSTRUCTIONS ON USE 
 
 
16. INFORMATION IN BRAILLE 
 
Jyseleca 100 mg 
 
 
17. UNIQUE IDENTIFIER – 2D BARCODE 
 
2D barcode carrying the unique identifier included. 
 
 
18. UNIQUE IDENTIFIER – HUMAN READABLE DATA 
 
PC 
SN 
NN 



28 

 
PARTICULARS TO APPEAR ON THE IMMEDIATE PACKAGING 
 
BOTTLE LABELLING FOR 100 MG FILM-COATED TABLETS 
 
 
1. NAME OF THE MEDICINAL PRODUCT 
 
Jyseleca 100 mg film-coated tablets 
filgotinib 
 
 
2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each film-coated tablet contains 100 mg filgotinib (as maleate). 
 
 
3. LIST OF EXCIPIENTS 
 
Contains lactose. 
 
 
4. PHARMACEUTICAL FORM AND CONTENTS 
 
30 film-coated 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 
 
Do not swallow the desiccant. 
 
 
8. EXPIRY DATE 
 
EXP 
 
 
9. SPECIAL STORAGE CONDITIONS 
 
Store in the original package in order to protect from moisture. Keep the bottle tightly closed. 
 
 



29 

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 Ireland UC 
Carrigtohill 
County Cork, T45 DP77 
Ireland 
 
 
12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/20/1480/001 30 film-coated tablets 
EU/1/20/1480/002 90 (3 bottles of 30) film-coated tablets 
 
 
13. BATCH NUMBER 
 
Lot 
 
 
14. GENERAL CLASSIFICATION FOR SUPPLY 
 
 
15. INSTRUCTIONS ON USE 
 
 
16. INFORMATION IN BRAILLE 
 
 
17. UNIQUE IDENTIFIER – 2D BARCODE 
 
 
18. UNIQUE IDENTIFIER – HUMAN READABLE DATA 
 
 



30 

 
PARTICULARS TO APPEAR ON THE OUTER PACKAGING 
 
CARTON LABELLING FOR 200 MG FILM-COATED TABLETS 
 
 
1. NAME OF THE MEDICINAL PRODUCT 
 
Jyseleca 200 mg film-coated tablets 
filgotinib 
 
 
2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each film-coated tablet contains 200 mg filgotinib (as maleate). 
 
 
3. LIST OF EXCIPIENTS 
 
Contains lactose. 
 
 
4. PHARMACEUTICAL FORM AND CONTENTS 
 
30 film-coated tablets 
 
90 (3 bottles of 30) film-coated tablets 
 
 
5. METHOD AND ROUTE(S) OF ADMINISTRATION 
 
Read the package leaflet before use. 
 
Oral use 
 
QR code to be included 
www.jyseleca.eu 
 
 
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 
 
Do not swallow the desiccant. 
 
 
8. EXPIRY DATE 
 
EXP 
 
 

http://www.jyseleca.eu/


31 

9. SPECIAL STORAGE CONDITIONS 
 
Store in the original package in order to protect from moisture. Keep the bottle tightly closed. 
 
 
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 Ireland UC 
Carrigtohill 
County Cork, T45 DP77 
Ireland 
 
 
12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/20/1480/003 30 film-coated tablets 
EU/1/20/1480/004 90 (3 bottles of 30) film-coated tablets 
 
 
13. BATCH NUMBER 
 
Lot 
 
 
14. GENERAL CLASSIFICATION FOR SUPPLY 
 
 
15. INSTRUCTIONS ON USE 
 
 
16. INFORMATION IN BRAILLE 
 
Jyseleca 200 mg 
 
 
17. UNIQUE IDENTIFIER – 2D BARCODE 
 
2D barcode carrying the unique identifier included. 
 
 
18. UNIQUE IDENTIFIER – HUMAN READABLE DATA 
 
PC 
SN 
NN 



32 

 
PARTICULARS TO APPEAR ON THE IMMEDIATE PACKAGING 
 
BOTTLE LABELLING FOR 200 MG FILM-COATED TABLETS 
 
 
1. NAME OF THE MEDICINAL PRODUCT 
 
Jyseleca 200 mg film-coated tablets 
filgotinib 
 
 
2. STATEMENT OF ACTIVE SUBSTANCE(S) 
 
Each film-coated tablet contains 200 mg filgotinib (as maleate). 
 
 
3. LIST OF EXCIPIENTS 
 
Contains lactose. 
 
 
4. PHARMACEUTICAL FORM AND CONTENTS 
 
30 film-coated 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 
 
Do not swallow the desiccant. 
 
 
8. EXPIRY DATE 
 
EXP 
 
 
9. SPECIAL STORAGE CONDITIONS 
 
Store in the original package in order to protect from moisture. Keep the bottle tightly closed. 
 
 



33 

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 Ireland UC 
Carrigtohill 
County Cork, T45 DP77 
Ireland 
 
 
12. MARKETING AUTHORISATION NUMBER(S) 
 
EU/1/20/1480/003 30 film-coated tablets 
EU/1/20/1480/004 90 (3 bottles of 30) film-coated tablets 
 
 
13. BATCH NUMBER 
 
Lot 
 
 
14. GENERAL CLASSIFICATION FOR SUPPLY 
 
 
15. INSTRUCTIONS ON USE 
 
 
16. INFORMATION IN BRAILLE 
 
 
17. UNIQUE IDENTIFIER – 2D BARCODE 
 
 
18. UNIQUE IDENTIFIER – HUMAN READABLE DATA 
 
 



34 

 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 

B. PACKAGE LEAFLET 
 
 



35 

Package leaflet: Information for the patient 
 

Jyseleca 100 mg film-coated tablets 
Jyseleca 200 mg film-coated tablets 

filgotinib 
 

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 Jyseleca is and what it is used for 
2. What you need to know before you take Jyseleca 
3. How to take Jyseleca 
4. Possible side effects 
5. How to store Jyseleca 
6. Contents of the pack and other information 
 
 
1. What Jyseleca is and what it is used for 
 
Jyseleca contains the active substance filgotinib. It belongs to a group of medicines called Janus kinase 
inhibitors, which help reduce inflammation. 
 
Jyseleca is used to treat adults with rheumatoid arthritis, an inflammatory disease of the joints. It 
can be used if previous therapy did not work well enough, or was not tolerated. Jyseleca can be used 
on its own, or together with another arthritis medicine, methotrexate. 
 
Jyseleca reduces inflammation in your body. It helps to reduce pain, tiredness, stiffness and 
swelling in your joints, and it slows down damage to the bone and cartilage in the joints. These effects 
can help you to perform your normal daily activities, and improve your quality of life. 
 
 
2. What you need to know before you take Jyseleca 
 
Do not take Jyseleca 
• if you are allergic to filgotinib or any of the other ingredients of this medicine (listed in 

section 6). 
• if you have active tuberculosis (TB). 
• if you have an active serious infection (see section “Warnings and precautions”). 
• if you are pregnant or think you may be pregnant. 
 
→ If any of these apply to you, do not take Jyseleca and tell your doctor immediately. 
 



36 

Warnings and precautions 
Talk to your doctor or pharmacist before taking Jyseleca: 
• if you have an infection, or if you often get infections. Tell your doctor if you become ill 

(especially with a fever or chills, shortness of breath, persistent cough, or tiredness) while you 
are taking Jyseleca. Jyseleca can reduce your body’s ability to fight infections. It may make an 
existing infection worse or increase the chance of you getting a new infection. If you are aged 
75 years or older, there is a higher risk of you getting a serious infection. 

• if you have ever had tuberculosis (TB), or have come into contact with somebody with TB. 
You may need tests to check for tuberculosis before and during treatment with Jyseleca. 

• if you have had a herpes zoster infection (shingles) in the past, Jyseleca can allow it to come 
back. Tell your doctor if you get a painful skin rash with blisters during Jyseleca treatment as 
these can be signs of shingles. 

• if you have ever had hepatitis B or C. 
• if you have cancer. Your doctor will have to decide if you can be given Jyseleca. 
• if you are at high risk of developing skin cancer, your doctor may recommend preventive 

measures such as regular skin examinations while taking Jyseleca. Talk to your doctor if you 
develop a new mark or any change in the appearance of an area on the skin. Some patients 
treated with Jyseleca have developed skin cancers. 

• if you are a man, Jyseleca may decrease your fertility (lower your ability to father a child) or 
cause infertility (inability to father a child). See also section “Male fertility”. 

• if you recently had a vaccine, or are due to have one. Certain types of vaccines (live vaccines) 
are not recommended while using Jyseleca. Talk to your doctor or pharmacist before you start 
Jyseleca. They may want to make sure that you are up to date with your vaccinations. 

• if you have heart problems, high blood pressure, or high cholesterol. 
• if you have had blood clots in the veins of your legs (deep vein thrombosis) or lungs 

(pulmonary embolism) in the past. Tell your doctor if you get a painful swollen leg, chest pain, 
or shortness of breath as these can be signs of blood clots in the veins. 

 
Children and adolescents 
Do not give this medicine to children and adolescents under 18 years of age because it has not been 
studied in this age group. 
 
Other medicines and Jyseleca 
Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines, 
especially if you use medicines that affect your immune system (such as azathioprine, ciclosporin and 
tacrolimus). 
It is also very important to talk to your doctor of pharmacist if you are taking any of the following: 
• medicines to treat heart failure, coronary disease or high blood pressure (such as digoxin, 

diltiazem, carvedilol or valsartan) 
• medicines to treat high cholesterol (such as fenofibrate or statins including atorvastatin, 

pravastatin or simvastatin) 
 
Pregnancy, contraception, breast-feeding and male fertility 
Pregnancy 
Jyseleca must not be used in pregnancy. If you are pregnant, think you may be pregnant or if you 
are planning to have a baby, do not take this medicine. Talk to your doctor for advice. 
 
Contraception 
Be careful not to get pregnant while you are taking Jyseleca. You must use reliable contraception 
while you are taking Jyseleca, and for at least 1 week after you take your last dose of Jyseleca. If you 
do become pregnant while you are taking Jyseleca, stop taking the tablets and tell your doctor 
immediately. 
 
Breast-feeding 
Do not breast-feed while you are taking Jyseleca. It is not known whether the active substance 
passes into human breast milk. 



37 

 
Male fertility 
If you are a man taking Jyseleca, it is possible that this medicine could affect your sperm production 
and may decrease your fertility (lower your ability to father a child) or cause infertility (inability to 
father a child). It is not known whether these effects could be temporary or permanent. Talk to your 
doctor if you have any questions or concerns about this. 
 
Driving and using machines 
Jyseleca can cause dizziness. If you feel dizzy when taking Jyseleca, do not drive and do not use any 
tools or machines. 
 
Jyseleca contains lactose 
Each Jyseleca 100 mg film-coated tablet contains 76 mg of lactose, and each Jyseleca 200 mg 
film-coated tablet contains 152 mg of lactose. If you have been told by your doctor that you have an 
intolerance to some sugars, contact your doctor before taking this medicine. 
 
 
3. How to take Jyseleca 
 
Always take this medicine exactly as your doctor has told you. Check with your doctor or pharmacist 
if you are not sure. 
 
The recommended dose is one 200 mg tablet once a day. 
 
If you are over 75 years old or if you have kidney problems, your doctor may recommend a dose of 
one 100 mg tablet once a day. Talk to your doctor if you have severe liver problems, as Jyseleca is not 
recommended for you. 
 
Swallow your tablet with a glass of water. Do not split, crush, or chew the tablet before swallowing as 
it may change how much medicine gets into your body. You can take Jyseleca with food or between 
meals. Do not swallow the desiccant. 
 
Take Jyseleca at the same time every day. This will help you to remember to take the tablets. 
 
Your doctor may stop treatment temporarily or permanently if blood tests show a low white or red 
blood cell count. 
 
If you take more Jyseleca than you should 
If you take more tablets than you should, tell your doctor straight away. 
 
If you forget to take Jyseleca 
• If you miss a dose, take it as soon as you remember. 
• If you have gone a whole day (24 hours) without taking a dose, just skip the missed dose and 

take a single dose at your usual time. 
• Do not take a double dose to make up for a forgotten tablet. 
 
If you stop taking Jyseleca 
If you stop taking Jyseleca, tell your doctor straight away. 
 
If you have any further questions on the use of this medicine, ask your doctor or pharmacist. 
 
 
4. Possible side effects 
 
Like all medicines, this medicine can cause side effects, although not everybody gets them. 
 



38 

Serious side effects 
Talk to your doctor or get medical help straight away if you get any signs of serious infection such as: 
• fever and symptoms of urinary tract infection (urinating more frequently than usual, pain or 

discomfort when urinating or back pain). Urinary tract infections are common (may affect up to 
1 in 10 people), and some of these may be serious. 

• lung infection (pneumonia): symptoms can include persistent cough, fever, shortness of breath, 
and tiredness. This is uncommon (may affect up to 1 in 100 people). 

• shingles (herpes zoster): symptoms can include a painful skin rash with blisters. This is 
uncommon (may affect up to 1 in 100 people). 

 
Other side effects 
Talk to your doctor if you notice any of the following side effects: 
 
Common 
(may affect up to 1 in 10 people) 
• throat and nose infections 
• dizziness 
• feeling sick (nausea). 
 
Uncommon 
(may affect up to 1 in 100 people) 
 
Blood tests may show: 
• a low number of white blood cells (neutrophils) 
• an increase in a muscle enzyme called creatine phosphokinase 
• an increased level of blood fat (cholesterol). 
 
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 Jyseleca 
 
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 carton and bottle after EXP. The 
expiry date refers to the last day of that month. 
 
Store in the original package in order to protect from moisture. Keep the bottle tightly closed. Do not 
use this medicine if you notice that the seal over the bottle opening is broken or missing. 
 
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 Jyseleca contains 
• The active substance is filgotinib. Each film-coated tablet contains 100 or 200 mg of filgotinib 

(as filgotinib maleate). 
 

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


39 

• The other ingredients are: 
Tablet core: microcrystalline cellulose, lactose monohydrate, pregelatinised starch, colloidal silicon 
dioxide, fumaric acid, magnesium stearate 
Film-coating: polyvinyl alcohol, titanium dioxide (E171), macrogol, talc, iron oxide yellow (E172), 
iron oxide red (E172) 
 
What Jyseleca looks like and contents of the pack 
Jyseleca 100 mg film-coated tablets are beige, 12 mm × 7 mm in size, capsule-shaped with “GSI” on 
one side and “100” on the other. 
 
Jyseleca 200 mg film-coated tablets are beige, 17 mm × 8 mm in size, capsule-shaped with “GSI” on 
one side and “200” on the other. 
 
Jyseleca 100 mg and 200 mg are available in bottles of 30 tablets and in packs made up of 3 bottles, 
each containing 30 tablets. Each bottle contains a silica gel desiccant that must be kept in the bottle to 
help protect your tablets. The silica gel desiccant is contained in a separate sachet or canister and 
should not be swallowed. 
 
Not all pack sizes may be marketed. 
 
Marketing Authorisation Holder 
Gilead Sciences Ireland UC 
Carrigtohill 
County Cork, T45 DP77 
Ireland 
 
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 
Galapagos Biopharma Belgium B.V. 
Tél/Tel: 00800 7878 1345 
 

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

България 
Gilead Sciences Ireland UC 
Тел.: + 353 (0) 1 686 1888 
 

Luxembourg/Luxemburg 
Galapagos Biopharma Belgium B.V. 
Tél/Tel: 00800 7878 1345 
 

Česká republika 
Gilead Sciences s.r.o. 
Tel: + 420 910 871 986 
 

Magyarország 
Gilead Sciences Ireland UC 
Tel.: + 353 (0) 1 686 1888 
 

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

Malta 
Gilead Sciences Ireland UC 
Tel: + 353 (0) 1 686 1888 
 

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

Nederland 
Galapagos Biopharma Netherlands B.V. 
Tel: 00800 7878 1345 
 



40 

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

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 
Galapagos Biopharma Spain, S.L. 
Tel: 00800 7878 1345 
 

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

France 
Galapagos SASU 
Tél : 00800 7878 1345 
 

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

Hrvatska 
Gilead Sciences Ireland UC 
Tel: + 353 (0) 1 686 1888 
 

România 
Gilead Sciences Ireland UC 
Tel: + 353 (0) 1 686 1888 
 

Ireland 
Gilead Sciences Ireland UC 
Tel: + 353 (0) 214 825 999 
 

Slovenija 
Gilead Sciences Ireland UC 
Tel: + 353 (0) 1 686 1888 
 

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

Slovenská republika 
Gilead Sciences Slovakia s.r.o. 
Tel: + 421 232 121 210 
 

Italia 
Galapagos Biopharma Italy S.r.l. 
Tel: 00800 7878 1345 
 

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

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

 
This leaflet was last revised in 
 
Detailed information on this medicine is available on the European Medicines Agency web site: 
http://www.ema.europa.eu. 
 
QR code to be included 
www.jyseleca.eu 

http://www.ema.europa.eu/
http://www.jyseleca.eu/

	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