Edurant (Rilpivirine Hydrochloride) - Summary

EDURANT SUMMARY

EDURANT (rilpivirine) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1). EDURANT is available as a white to off-white, film-coated, round, biconvex, 6.4 mm tablet for oral administration. Each tablet contains 27.5 mg of rilpivirine hydrochloride, which is equivalent to 25 mg of rilpivirine.

EDURANT™, in combination with other antiretroviral agents, is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in antiretroviral treatment-naive adult patients.

This indication is based on Week 48 safety and efficacy analyses from 2 randomized, double-blind, active controlled, Phase 3 trials in treatment-naive subjects and Week 96 safety and efficacy analyses from a Phase 2b trial in treatment-naive subjects [see Clinical Studies].

The following points should be considered when initiating therapy with EDURANT:

• More EDURANT treated subjects with HIV-1 RNA greater than 100,000 copies/mL at the start of therapy experienced virologic failure compared to subjects with HIV-1 RNA less than 100,000 copies/mL at the start of therapy [ see Clinical Studies ].
• The observed virologic failure rate in EDURANT treated subjects conferred a higher rate of overall treatment resistance and cross-resistance to the NNRTI class compared to efavirenz [ see Clinical Pharmacology ].
• More subjects treated with EDURANT developed lamivudine/emtricitabine associated resistance compared to efavirenz [ see Clinical Pharmacology ].

NEWS HIGHLIGHTS

Published Studies Related to Edurant (Rilpivirine)

Rilpivirine: a second-generation nonnucleoside reverse transcriptase inhibitor. [2012]
CONCLUSION: Rilpivirine is a viable NNRTI for HIV-infected patients who have not

Efficacy and safety of rilpivirine (TMC278) versus efavirenz at 48 weeks in treatment-naive HIV-1-infected patients: pooled results from the phase 3 double-blind randomized ECHO and THRIVE Trials. [2012]
THRIVE trials comparing rilpivirine (TMC278) and efavirenz... CONCLUSIONS: At week 48, rilpivirine 25 mg once daily and efavirenz 600 mg once

Rilpivirine versus efavirenz with tenofovir and emtricitabine in treatment-naive adults infected with HIV-1 (ECHO): a phase 3 randomised double-blind active-controlled trial. [2011]
with tenofovir-disoproxil-fumarate and emtricitabine... INTERPRETATION: Rilpivirine showed non-inferior efficacy compared with efavirenz,

A compartmental pharmacokinetic evaluation of long-acting rilpivirine in HIV-negative volunteers for pre-exposure prophylaxis. [2014]
Rilpivirine long-acting (RPV-LA) is a parenteral formulation enabling prolonged plasma exposure... PK and viral inhibition of repeated doses will be important in further dose selection.

Impact of food and different meal types on the pharmacokinetics of rilpivirine. [2013]
The objective of the study was to determine the impact of food and different meal types on the pharmacokinetics of rilpivirine, a nonnucleoside reverse transcriptase inhibitor. In this open-label, randomized, crossover study, healthy volunteers received a single, oral 75 mg dose of rilpivirine either with a normal-fat breakfast (reference), under fasting conditions, with a high-fat breakfast, or with a protein-rich nutritional drink...

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Clinical Trials Related to Edurant (Rilpivirine)

A Study of TMC278 in Human Immunodeficiency Virus Type 1 Infected Patients, Who Are Not Treated With Antiretroviral Medicines [Completed]
The purpose of this study is to evaluate the dose-response relationship of antiviral activity after 48 weeks treatment with 3 different dose regimens of TMC278.

A Study to Evaluate Safety, Acceptability, Pharmacokinetics, and ex Vivo Pharmacodynamics of TMC278 Long Acting Formulation in HIV-1 Seronegative Participants [Recruiting]
The purpose of this study is to evaluate the safety, acceptability, pharmacokinetics (what the body does to the medication), and ex vivo (tested outside the body) pharmacodynamics (what the medication does to the body) of TMC278 long acting (slowly effective after initial dosage and maintaining its effects over a long period of time) when administered as an intramuscular (ie, in to the muscle) injection in adult participants who are seronegative for human immunodeficiency virus type 1 (HIV-1).

A Study to Investigate the Safety, Tolerability and Pharmacokinetics of Repeat Dose Administration of Long-Acting GSK1265744 and Long-Acting TMC278 Intramuscular and Subcutaneous Injections in Healthy Adult Subjects [Completed]
LAI115428 is a Phase I, randomized, repeat dose escalation study to determine the safety, tolerability, and PK profile of intramuscular and subcutaneous injections of GSK1265744 in a long acting parenteral (LAP) formulation in healthy subjects. Subjects will be randomized to 3 monthly dosing cohorts and 1 quarterly dosing cohort with either intramuscular or subcutaneous dosing. In the monthly dosing cohorts subjects will receive GSK1265744 alone for 2 months and then in combination with TMC278 long acting parenteral (LA) for 2 months. For the quarterly dosing cohort, 2 quarterly intramuscular doses of GSK1265744 LAP will be given alone. Three dose levels of GSK1265744 will be evaluated partly in combination with TMC278 LA to adequately characterize the GSK1265744 LAP and TMC278 LA safety, tolerability, and PK profile. A total enrolment of approximately 40 healthy subjects is planned for this study.

The Rilpivirine Cerebrospinal-fluid (CSF) Study [Completed]
This is a phase I pharmacokinetic study of HIV positive patients stable on antiretroviral therapy who will switch treatment when enrolled from nevirapine to rilpivirine. On day 60 of the study the participants will attend clinic where they will have blood collected followed by a lumbar puncture where cerebrospinal fluid will be collected to measure drug concentration. The participants will then restart their original regime with nevirapine.

A Study to Investigate the Effect of Steady-State TMC278 on the Pharmacokinetics of a Single Dose of Digoxin [Completed]
The purpose of this study is to investigate the effect of steady-state (constant concentration of medication in the blood) TMC278 on the single dose pharmacokinetics (what the body does to the medication) of digoxin.

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Reports of Suspected Edurant (Rilpivirine) Side Effects

Pyrexia (6),  Rash Generalised (6),  Abortion Spontaneous (4),  Cystic Lymphangioma (4),  Renal Failure Acute (4),  Loss of Consciousness (3),  Blood Creatinine Increased (3),  Nausea (3),  Blood Triglycerides Increased (1),  CD4 Lymphocytes Decreased (1), more >>