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.
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Authors | Paul L McCormack |
Journal | Drugs
(Drugs)
Vol. 74
Issue 11
Pg. 1241-52
(Jul 2014)
ISSN: 1179-1950 [Electronic] New Zealand |
PMID | 25005775
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
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Chemical References |
- HIV Integrase Inhibitors
- Heterocyclic Compounds, 3-Ring
- Oxazines
- Piperazines
- Pyridones
- dolutegravir
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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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