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

Abstract

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.

Keywords:

• drug-to-drug interactions
• pharmacodynamic
• pharmacokinetic
• raltegravir
• resistance

Declaration of interest

A Calcagno has received travel grants or speaker’s honoraria from Abbott, Bristol-Myers Squibb, Merck Sharp & Dohme and Janssen-Cilag. S Bonora has received grants, travel grants and consultancy fees from Abbott, Bristol-Myers Squibb, Gilead Sciences, GlaxoSmithKline, Merck Sharp & Dohme, Pfizer and Janssen-Cilag. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.