Raltegravir: a review of its pharmacokinetics, pharmacology and clinical studies.

IMPORTANCE OF THE FIELD: Raltegravir is the first HIV-integrase inhibitor licensed by the FDA. AREAS COVERED IN THIS REVIEW: A PubMed search was conducted for all published reports up to 1 May 2010 related to raltegravir pharmacokinetics, pharmacology, drug-drug interactions and clinical studies in HIV-infected patients. Also included in this review are the updated European and US Prescriber's Information (European Medicines Agency and the FDA) and abstracts from recent international scientific meetings. WHAT THE READER WILL GAIN: After reading the review, a thorough insight in raltegravir pharmacokinetics and pharmacology will be obtained, as well as an up-to-date overview of all published drug-drug interaction studies. Furthermore, one should be able to make an evidence-based opinion on the drug's clinical efficacy and tolerability. TAKE HOME MESSAGE: Raltegravir is a welcome addition to the antiretroviral drug armamentarium due to its good tolerability, low potential for drug-drug interactions and good clinical efficacy in both treatment-naive and -experienced patients.