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

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

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Adis, Level 1, 5 The Warehouse Way, Northcote 0627; Private Bag 65901, Mairangi Bay 0754, Auckland, New Zealand,


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.

[Indexed for MEDLINE]

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