Pharmacologic characteristics of investigational and recently approved agents for the treatment of HIV

PURPOSE OF REVIEW: Two agents from antiretroviral classes with novel mechanisms of action against HIV received regulatory approval in 2007. Maraviroc is the first in the class of chemokine coreceptor 5 antagonists and raltegravir is the first in the class of integrase inhibitors. There are other compounds in these two new classes in later stages of clinical development, as well as several protease inhibitors and nonnucleoside reverse transcriptase inhibitors that have been recently approved or are under investigation for use in treatment-experienced patients. The purpose of this article is to review the pharmacologic characteristics of these newly approved and investigational antiretroviral drugs, with particular emphasis on data presented or published within the past year. RECENT FINDINGS: Several pivotal studies describing the efficacy, safety, and pharmacologic properties of maraviroc, vicriviroc, etravirine, rilpivirine, raltegravir, elvitegravir, darunavir/ritonavir, and tipranavir/ritonavir have begun to emerge. SUMMARY: To date, these agents have demonstrated promising virologic activity with primarily excellent tolerability, but there is still much to learn about their pharmacology. Future studies should evaluate their potential for drug-drug interactions and elucidate their concentration-effect relationships. An appreciation for the pharmacology of these drugs is critical to their optimal use.