Pharmacokinetic and pharmacodynamic evaluation of raltegravir and experience from clinical trials in HIV-positive patients.

INTRODUCTION

Raltegravir was the first available integrase inhibitor for treating HIV-positive patients. This review aims to provide an overview of its role in the management of HIV-1 infection, highlighting its key pharmacokinetic and pharmacodynamic properties.

AREAS COVERED: This review covers material searched and obtained through Medline and PubMed up to April 2015.

EXPERT OPINION: Raltegravir for its tolerability, efficacy, few drug-to-drug interactions and for the amount of available data in difficult subgroups of patients is a key drug in the antiretroviral armamentarium. For its weak genetic barrier to resistance and erratic pharmacokinetic profile, it should be administered twice daily and with fully active companion antiretrovirals.