Pharmacokinetic evaluation of etravirine

Abstract

Importance of the field: Successful long-term treatment of HIV is hindered by development of resistance and providing active regimens for treatment-experienced patients remains challenging. Development of antiretrovirals active against resistant virus, such as the diarylpyrimidine non-nucleoside reverse transcriptase inhibitor (NNRTI) etravirine, is important to broaden treatment options to patients who have few available.

Areas covered in this review: We summarise pharmacology, pharmacokinetics, drug–drug interactions and clinical data of etravirine based on a PubMed search between 01 January 2003 and 01 September 2010 as well as relevant information from conference proceedings and the latest Summary of Product Characteristics and US Prescribing Information.

What the reader will gain: The reader will gain a comprehensive overview of etravirine clinical pharmacology, drug–drug interactions and mechanism of action. Information regarding efficacy, safety and tolerability in specific patients groups is provided to allow the reader to form an opinion regarding the role of etravirine in clinical practice.

Take home message: Etravirine, along with other new antiretrovirals, has widened treatment options for patients with multi-drug resistance. Etravirine is well tolerated with the majority of drug–drug interactions manageable and is effective in triple-class experienced patients. Clinical studies investigating etravirine in treatment-naive patients are ongoing to further clarify its safety and resistance profile.

Keywords::

• efficacy
• etravirine
• HIV
• non-nucleoside reverse transcriptase inhibitor
• pharmacokinetics