Integrase Inhibitors: After 10 Years of Experience, Is the Best Yet to Come?

Pharmacotherapy. 2019 May;39(5):576-598. doi: 10.1002/phar.2246. Epub 2019 Apr 1.

Abstract

The era of the integrase strand transfer inhibitors (INSTIs) for the treatment of human immunodeficiency virus (HIV) infection began with raltegravir in 2007. Since that time, several other INSTIs have been introduced including elvitegravir, dolutegravir, and, most recently, bictegravir, that have shown great utility as part of antiretroviral regimens in both treatment-naive and treatment-experienced patients. At present, antiretroviral guidelines fully endorse the INSTI class as part of all first-line treatment regimens. After 10 years of experience with INSTIs, newer agents are on the horizon such as cabotegravir and MK-2048 for potential use as either HIV pre-exposure prophylaxis or maintenance therapy. This review provides a brief overview of the INSTI class including agents currently available and those still in development, reviews available data from both completed and ongoing clinical trials, and outlines simplification strategies using INSTIs.

Keywords: HIV; Integrase inhibitors; antiretroviral therapy.

Publication types

  • Review

MeSH terms

  • Drug Interactions
  • HIV Infections / drug therapy*
  • HIV Infections / enzymology
  • HIV Integrase Inhibitors / administration & dosage
  • HIV Integrase Inhibitors / adverse effects
  • HIV Integrase Inhibitors / pharmacokinetics
  • HIV Integrase Inhibitors / therapeutic use*
  • Humans
  • Pre-Exposure Prophylaxis / methods*
  • Randomized Controlled Trials as Topic
  • Treatment Outcome

Substances

  • HIV Integrase Inhibitors