dolutegravir

Dolutegravir (GSK1349572) (IC50=2.7 nM), a two-metal-binding HIV integrase inhibitor, exhibits medium activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S Q148H.

Dolutegravir intermediate-1 (1-(2,2-dimethoxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid) is a new synthetic Dolutegravir intermediate. Dolutegravir is an integrase inhibitor developed for the treatment of human immunodeficiency virus (HIV)-1 infection.

Dolutegravir sodium (GSK-1349572A) salt(DTG; GSK1349572) is an HIV integrase inhibitor(IC50: 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S Q148H.

Dolutegravir M1 is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed primarily by the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1B1. 1.Zhu, J., Wang, P., Li, F., et al.CYP1A1 and 1B1-mediated metabolic pathways of dolutegravir, an HIV integrase inhibitorBiochem. Pharmacol.158174-184(2018)

Dolutegravir RR Isomer is an isomer of Dolutegravir -- a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.

Dolutegravir SR Isomer is an isomeric derivative of Dolutegravir -- a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.

Dolutegravir O-β-D-glucuronide is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed from dolutegravir primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A1in vivobut is also metabolized by UGT1A9 in human liver and kidney microsomes and UGT1A3 in human intestinal microsomes.2,1 1.Liu, S.N., Lu, J.B., Watson, C.J.W., et al.Mechanistic assessment of extrahepatic contributions to glucuronidation of integrase strand transfer inhibitorsDrug Metab. Dispos.47(5)535-544(2019) 2.Reese, M.J., Savina, P.M., Generaux, G.T., et al.In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitorDrug Metab. Dispos.41(2)353-361(2013)

Baloxavir (S-033447) is a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit.