Clinical trial NCT01121809: Plasma and Intracellular Concentrations of Raltegravir and Etravirine Administered Once Daily
Official title: Plasma and Intracellular Concentrations of Raltegravir and Etravirine Administered Once Daily (800 mg and 400 mg, Respectively) Compared With Standard Dosing (400 mg and 200 mg/12 h) in Patients With HIV Infection
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE4
Conditions: HIV-1 Infection
HIV Infections
Keywords: Raltegravir
etravirine
pharmacokinetics
intracellular
Lead sponsor: Hospitales Universitarios Virgen del Rocío
Sponsor class: OTHER
First posted: 2010-05-12
Enrollment: 16
Sex: ALL
Minimum age (years): 18
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: no
Allocation: NON_RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: TREATMENT

Brief summary: Hypothesis: the intracellular concentrations of raltegravir (RAL) and etravirine (ETV) administrated as 800 and 400 mg once a day, respectively, are similar to those obtained with the standard doses of 400 and 200 mg/12h, respectively.

Objective: To analyze the plasma and intracellular concentrations of RAL and ETV administrated as 800 and 400 mg once daily respectively compared with standard doses of 400 and 200 mg/12h, respectively, and if they support its once daily administration.

Detailed description: Objective: To analyze the plasma and intracellular concentrations of RAL and ETV administrated as 800 and 400 mg once daily respectively compared with standard doses of 400 and 200 mg/12h, respectively, and if they support its once daily administration.

Method: Phase IV, prospective, open labelled clinical trial with a planned duration of 24 weeks in which 16 patients from Hospitales Universitarios Virgen del Rocío will be enrolled. A 12 hours pharmacokinetic profile (immediately before and after 1, 2, 3, 4, 6, 8, 10 and 12 h) will be obtained after a supervised drug intake while taking RAL or ETV bid. Afterwards,the patients will take RAL or ETV once a day for 7 - 10 days. Subsequently, a new pharmacokinetic profile (predose and after 1, 2, 3, 4, 6, 8, 10, 12, 16, 20 and 24 h after a supervised drug intake) will be obtained.

Eligibility criteria: Inclusion Criteria:

* Adult HIV-1-infected patients taking raltegravir- or etravirine-based antiretroviral regimens

Exclusion Criteria:

* Pregnancy
* Concomitant use of drugs that have potential interactions with raltegravir or etravirine pharmacokinetics
* Cirrhosis with clinical or analytic data of liver failure.
* Clinical history suggesting malabsorption or presence of diarrhea (\> 3 stools / day) that could interfere with the absorption of study drugs.

Primary outcomes:
measure: Changes in pharmacokinetic parameters (Cmax, Cmin, AUC, t1/2, and Cl), both in plasma and intracellular, of RAL and ETV.
timeFrame: baseline and 1 week
Secondary outcomes:
Other outcomes:
Locations:
city: Sevilla
country: Spain
facility: Hospitales Universitarios Virgen del Rocio
Study officials:
affiliation: Hospitales Universitarios Virgen del Rocío
name: Luis F Lopez-Cortes, ND, PhD
role: PRINCIPAL_INVESTIGATOR
References:
citation: Gutierrez-Valencia A, Martin-Pena R, Torres-Cornejo A, Ruiz-Valderas R, Castillo-Ferrando JR, Lopez-Cortes LF. Intracellular and plasma pharmacokinetics of 400 mg of etravirine once daily versus 200 mg of etravirine twice daily in HIV-infected patients. J Antimicrob Chemother. 2012 Mar;67(3):681-4. doi: 10.1093/jac/dkr534. Epub 2011 Dec 21.