Dolutegravir: a review of its use in the management of HIV-1 infection in adolescents and adults

Drugs. 2014 Jul;74(11):1241-52. doi: 10.1007/s40265-014-0256-y.

Abstract

Dolutegravir (Tivicay(®)) is a new-generation HIV-1 integrase strand transfer inhibitor recently approved in the EU and Japan for the treatment of HIV-1 infection in adolescents and adults in combination with other antiretroviral drugs. It is suitable for once-daily administration and achieves therapeutic concentrations without the need for pharmacokinetic boosting. It has a high barrier to resistance and is generally active against viral strains resistant to first-generation integrase inhibitors. In well-designed clinical trials in treatment-naive or treatment-experienced, integrase inhibitor-naive patients, dolutegravir-based combinations were shown to be noninferior or superior to raltegravir-based combinations, an efavirenz-based combination and ritonavir-boosted darunavir-based combinations with respect to virological suppression (plasma HIV-1 RNA <50 copies/mL) at week 48. Dolutegravir was also effective in a high proportion of patients failing on raltegravir- or elvitegravir-based therapy as a result of integrase resistance mutations. Dolutegravir was generally well tolerated, with the vast majority of adverse events being mild or moderate in intensity; serious adverse events were uncommon. Therefore, dolutegravir is an important new addition to the expanding list of antiretroviral drugs for treating HIV-1 infection in adults and adolescents.

Publication types

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

MeSH terms

  • Adolescent
  • Adult
  • Clinical Trials as Topic / methods
  • Disease Management
  • HIV Infections / diagnosis
  • HIV Infections / drug therapy*
  • HIV Integrase Inhibitors / therapeutic use*
  • HIV-1*
  • Heterocyclic Compounds, 3-Ring / therapeutic use*
  • Humans
  • Oxazines
  • Piperazines
  • Pyridones

Substances

  • HIV Integrase Inhibitors
  • Heterocyclic Compounds, 3-Ring
  • Oxazines
  • Piperazines
  • Pyridones
  • dolutegravir