DOLUTEGRAVIR, AN HIV INTEGRASE INHIBITOR FOR THE TREATMENT OF HIV INFECTION

Dolutegravir, a next-generation integrase strand transfer inhibitor, was recently approved by the United States Food and Drug Administration to treat antiretroviral therapy-naive as well as treatment-experienced HIV-infected individuals, including those who have been treated with other integrase strand transfer inhibitors. Dolutegravir is the first stand-alone agent in its class, with a pharmacokinetic profile that allows once-daily administration without the requirement for pharmacologic boosting. It is metabolized primarily by UDP-glucuronosyltransferase 1-1 (UGT1A1) and is expected to have a limited propensity for drug-drug interactions. Furthermore, dolutegravir retains significant virologic activity against raltegravir- or elvitegravir-associated HIV-1 resistance mutations.