Dolutegravir (DTG), a novel integrase strand transfer inhibitor (INSTI), is
one of the newest addition to the arsenal of anti-human immunodeficiency virus
(HIV) therapeutics. Dolutegravir is the first member of the class of second generation
integrase strand transfer inhibitors aimed primarily to address the current unmet need
for novel unboosted integrase inhibitors with convenient once-daily dosing and a
superior resistance profile. During its clinical development, DTG has demonstrated
noninferior or superior efficacy in both treatment-naive as well as treatmentexperienced
individuals including those who have previously failed first generation
INSTIs. Other potential advantages include a favorable safety profile, low propensity
for drug-drug interactions, and prolonged serum half-life permitting once-daily
administration in treatment-naive or treatment-experienced INSTI naive HIV patients. Twice-daily
administration is recommended in individuals with established or suspected resistance to first-generation
INSTIs. This review outlines the need for new HIV therapeutics and summarizes the efficacy, safety, and
pharmacokinetic profile of dolutegravir.
Keywords: Dolutegravir, integrase inhibitor, integrase strand transfer inhibitor, antiretroviral therapy.
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