Drug safety profile of integrase strand transfer inhibitors

Expert Opin Drug Saf. 2014 Apr;13(4):431-45. doi: 10.1517/14740338.2014.897327. Epub 2014 Mar 6.

Abstract

Introduction: HIV-1 integrase strand transfer inhibitors (INSTIs) are a novel class of antiretroviral drugs with a good safety profile. Several INSTIs have been developed clinically.

Areas covered: The purpose of this review is to examine the safety data of the three FDA-approved INSTIs: Raltegravir (RAL), Elvitegravir (EVG) and Dolutegravir (DTG). The most relevant papers related to the safety profile of integrase inhibitors were selected and summarized.

Expert opinion: INSTIs have demonstrated a favorable safety profile in Phase II and III trials. The most common clinical adverse events reported were diarrhea, nausea and headache. DTG and cobicistat, a component of Stribild(™), increase serum creatinine and decrease estimated creatinine clearance due to inhibition of active tubular secretion of creatinine without affecting renal glomerular function. INSTIs intrinsic potency, together with an outstanding safety profile, preludes an important role for these drugs to build up highly active antiretroviral treatment (HAART) in the near future.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Anti-Retroviral Agents / adverse effects*
  • Anti-Retroviral Agents / therapeutic use
  • Clinical Trials, Phase II as Topic
  • Clinical Trials, Phase III as Topic
  • HIV Infections / drug therapy
  • HIV Integrase / metabolism*
  • HIV Integrase Inhibitors / adverse effects*
  • HIV Integrase Inhibitors / therapeutic use
  • Humans
  • Safety

Substances

  • Anti-Retroviral Agents
  • HIV Integrase Inhibitors
  • HIV Integrase