Institutional members access full text with Ovid®

Share this article on:

Long-acting antiviral agents for HIV treatment

Margolis, David A.; Boffito, Marta

Current Opinion in HIV & AIDS: July 2015 - Volume 10 - Issue 4 - p 246–252
doi: 10.1097/COH.0000000000000169

Purpose of review: Long-acting antiretroviral (ARV) agents are currently under development for the treatment of chronic HIV infection. This review focuses on data recently produced on injectable ARVs for patients living with HIV/AIDS and on the patients’ perspectives on the use of these agents.

Recent findings: Crystalline nanoparticle formulations of the nonnucleoside reverse transcriptase inhibitor rilpivirine (TMC278) and of the HIV-1 integrase strand transfer inhibitor cabotegravir (GSK1265744) have progressed into phase II clinical trials as injectable maintenance therapy for patients living with HIV/AIDS with an undetectable viral load.

Summary: Phase II studies evaluating the coadministration of rilpivirine and cabotegravir intramuscularly to HIV-infected individuals with an undetectable viral load are currently underway. Rilpivirine and cabotegravir are characterized by different mechanisms of action against HIV and a favorable drug interaction profile, providing a rationale for coadministration. The high potency and low daily dosing requirements of oral cabotegravir and rilpivirine facilitate long-acting formulation development. Intramuscular dosing is preceded by an oral lead-in phase to assess safety and tolerability in individual participants. In addition to assessing the safety of injectable therapies in ongoing studies, it will be important to evaluate whether differences in drug adherence between injectable and oral therapies lead to different virologic outcomes, including rates of virologic failure and the emergence of resistance. Long-acting formulations may be associated with challenges, such as the management of adverse effects with persistent drug concentrations and the risk of virologic resistance, as drug concentrations decline following discontinuation.

aGlaxoSmithKline, Research Triangle Park, North Carolina, USA

bSt Stephen's Centre, Chelsea and Westminster Foundation Trust

cImperial College, London, UK

Correspondence to David A. Margolis, MD, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709 USA. Tel: +1 919 766 0755; e-mail:

This is an open-access article distributed under the terms of the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License, where it is permissible to download and share the work provided it is properly cited. The work cannot be changed in any way or used commercially.

Copyright © 2015 Wolters Kluwer Health, Inc. All rights reserved.