Recent Advances in Antiretroviral Agents: Potent Integrase Inhibitors

Title:Recent Advances in Antiretroviral Agents: Potent Integrase Inhibitors

Volume: 23 Issue: 18

Author(s): Mina Psichogiou*, Garyphalia Poulakou, Dimitrios Basoulis, Dimitrios Paraskevis, Antonios Markogiannakis and George L. Daikos

Affiliation:

• 1st Internal Medicine Department, Laiko General Hospital, National and Kapodistrian University of Athens, Agiou Thoma 17, Goudi, Athens,Greece

Keywords: Integrase strand transfer inhibitors, HIV, pharmacokinetics, efficacy, resistance, adherence, tolerability.

Abstract: Integrase strand transfer inhibitors (INSTIs) belong to a novel class of antiretroviral agents that have emerged as the new first-line treatments. Three such compounds are currently available, raltegravir, elvitegravir, dolutegravir and two more under development, bictegravir and cabotegravir. These compounds share the same mode of action but exhibit different pharmacokinetic/ pharmacodynamic properties, and drug-drug interactions. A series of studies in the past decade have established their efficacy compared to previous regimens, both in treatment- naïve and experienced patients. INSTIs have demonstrated a favorable safety profile with fewer adverse events and low rates of virological failure. Emergence of resistance to these agents, however, is a worrying concern, particularly for elvitegravir and raltegravir that display a lower genetic barrier than dolutegravir. On-going trials aim at establishing INSTIs as part of dual-drug HIV treatments or even monotherapy. New long-acting, injectable formulations are under investigation for treatment or prevention.

Cite this article as:

Psichogiou Mina *, Poulakou Garyphalia, Basoulis Dimitrios, Paraskevis Dimitrios, Markogiannakis Antonios and Daikos L. George, Recent Advances in Antiretroviral Agents: Potent Integrase Inhibitors, Current Pharmaceutical Design 2017; 23 (18) . https://dx.doi.org/10.2174/1381612823666170329142059