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

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.
AuthorsPaul L McCormack
JournalDrugs (Drugs) Vol. 74 Issue 11 Pg. 1241-52 (Jul 2014) ISSN: 1179-1950 [Electronic] New Zealand
PMID25005775 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
Chemical References
  • HIV Integrase Inhibitors
  • Heterocyclic Compounds, 3-Ring
  • Oxazines
  • Piperazines
  • Pyridones
  • dolutegravir
Topics
  • Adolescent
  • Adult
  • Clinical Trials as Topic (methods)
  • Disease Management
  • HIV Infections (diagnosis, drug therapy)
  • HIV Integrase Inhibitors (therapeutic use)
  • HIV-1
  • Heterocyclic Compounds, 3-Ring (therapeutic use)
  • Humans
  • Oxazines
  • Piperazines
  • Pyridones

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