Format

Send to:

Choose Destination
See comment in PubMed Commons below
Expert Opin Investig Drugs. 2009 Jul;18(7):1035-41. doi: 10.1517/13543780903055056.

Rilpivirine: a novel non-nucleoside reverse transcriptase inhibitor.

Author information

  • 1Clinical Research Fellow, Imperial College London, Division of Medicine, Ground Floor, Clinical Trials, Winston Churchill Wing, London W21PG, London, UK. l.garvey@imperial.ac.uk

Abstract

Combination antiretroviral therapy has transformed the prognosis and life expectancy of HIV-1 infected individuals in resource-rich settings. British guidelines currently recommend the non-nucleoside reverse transcriptase inhibitor (NNRTI) efavirenz as part of first-line treatment in therapy-naive HIV-1 infected individuals. However, efavirenz is limited by its low genetic barrier to the development of resistance, together with its potential for CNS toxicities. To overcome these obstacles, several 'next-generation' NNRTIs are in various stages of clinical development. Here, we review the journey of rilpivirine (also known as TMC278, Tibotec), from the discovery of the chemical compound, through successful Phase I and II development, to its current position of being studied in international Phase III trials for the treatment of therapy-naive HIV-1 infected subjects using a 25 mg daily dose. Pharmacokinetic findings and food and drug interactions are discussed, together with safety profile. Rilpivirine has demonstrated high antiviral activity (including against NNRTI-resistant isolates) in vitro, with similar rates of virological suppression in therapy-naive individuals at 96 weeks when compared to efavirenz. Rilpivirine seems to be well tolerated with less CNS disturbance than efavirenz, and has non-teratogenic potential; however, unfavorable interactions with acid suppressant medications will require heightened vigilance when rilpivirine is used in widespread clinical practice.

PMID:
19548857
[PubMed - indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Informa Healthcare
    Loading ...
    Write to the Help Desk