Dolutegravir sodium is an HIV integrase inhibitor (IC50= 2.7 nM) with modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.
Dolutegravir sodium (S/GSK1349572 sodium) is a potent, orally available inhibitor of HIV integrase strand transfer, exhibiting an IC50 of 2.7 nM against HIV-1 integrase-mediated strand transfer. It effectively suppresses HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium also maintains high efficacy against HIV-1 mutants Y143R, N155H, and G140S/Q148H, with EC50 values ranging from 3.6 to 5.8 nM[1][2].
Dolutegravir sodium/度鲁特韦钠盐 动物研究
Animal study
After a single intravenous (IV) administration, Dolutegravir shows low plasma clearance in rats (0.23 mL/min/kg) and monkeys (2.12 mL/min/kg). Both species exhibit similar half-lives of approximately 6 hours, and the steady-state volume of distribution (VSS) is low. Following oral administration, Dolutegravir is rapidly absorbed with high oral bioavailability when given as a solution to fasted male rats and a single monkey (75.6% and 87.0%, respectively). The exposure to Dolutegravir (Cmax and AUC) increases with rising doses when administered orally as a suspension to non-fasted rats up to 250 mg/kg and non-fasted monkeys up to 50 mg/kg, although the increase is less than proportional[2].
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