Title:Novel Second Generation HIV Integrase Inhibitor-DOLUTEGRAVIR: An Emerging Weapon Against HIV
Volume: 14
Issue: 3
Author(s): Vivek Jain, Diksha Gupta, Ashutosh Pareek and Yashumati Ratan
Affiliation:
Keywords:
Integrase inhibitor, dolutegravir, S/GSK-1349572, HIV.
Abstract: In antiretroviral therapy Integrase Inhibitors (INIs) have become a key component since
the approval of raltegravir in 2007 followed by the recent approval of elvitegravir in 2012. The next
generation compound dolutegravir has obtained the approval from USFDA in August 2013. Dolutegravir
possesses distinct characteristics like prolonged half-life, once-daily dosing without the need
for any booster along with no significant effect of food on its pharmacokinetics. Earlier reports have
shown that H51Y and R263K define a unique resistance pathway for dolutegravir. Dolutegravir is
effective in both initial therapy and in the salvage of many patients who display resistance to both
raltegravir and elvitegravir. Furthermore, due to its favorable metabolic profile and, without any dose
adjustment, it can be co-administered with most of the other approved antiretroviral agents. These
characteristics of dolutegravir along with reports from various ongoing phase III trials showed that it
can be a promising investigational drug for future clinical uses. This review focuses on recent data of
dolutegravir from well-designed clinical trials, resistance, with comparative drug interaction of various
INIs.
