Dolutegravir: an exciting new kid on the block

Expert Opin Pharmacother. 2014 Mar;15(4):573-82. doi: 10.1517/14656566.2014.868883. Epub 2014 Jan 22.

Abstract

Introduction: Dolutegravir is the first second-generation integrase inhibitor approved for the treatment of naïve as well as experienced HIV-infected individuals.

Areas covered: Data from pharmacokinetics, efficacy, safety, tolerability and resistance are reviewed from in vitro studies, Phase II and III clinical trials published in PubMed (Dolutegravir; S/GSK1349572) or presented in international meetings.

Expert opinion: Data from studies and clinical trials indicate that dolutegravir is safe, well tolerated and highly efficacious in the treatment of both antiretroviral-naïve and treatment-experienced patients and appears to have a higher genetic barrier to resistance than first-generation integrase inhibitors.

Publication types

  • Review

MeSH terms

  • Clinical Trials, Phase II as Topic
  • Clinical Trials, Phase III as Topic
  • Drug Resistance, Viral / genetics
  • Genetic Therapy
  • HIV Infections / drug therapy*
  • HIV Infections / enzymology
  • HIV Integrase / chemistry
  • HIV Integrase / genetics
  • HIV Integrase / metabolism
  • HIV Integrase Inhibitors / pharmacokinetics
  • HIV Integrase Inhibitors / therapeutic use*
  • Heterocyclic Compounds, 3-Ring / pharmacokinetics
  • Heterocyclic Compounds, 3-Ring / therapeutic use*
  • Humans
  • Mutation
  • Oxazines
  • Piperazines
  • Protein Conformation
  • Pyridones

Substances

  • HIV Integrase Inhibitors
  • Heterocyclic Compounds, 3-Ring
  • Oxazines
  • Piperazines
  • Pyridones
  • dolutegravir
  • HIV Integrase
  • p31 integrase protein, Human immunodeficiency virus 1