Pharma & Specialty Chemical Standards

Dolutegravir (IUPAC name: 4'-cyano-5-(2,4-difluorophenyl)-2,2'-bipyridine-3-carboxamide; molecular formula C17H11FN4O, molecular weight 306.3 g/mol) is an integrase strand transfer inhibitor (INSTI) with a bipyridine core and a difluorophenyl substituent. It exhibits high oral bioavailability, moderate lipophilicity, and a pKa of ~5.5. Therapeutically, it targets HIV-1 integrase, blocking viral DNA integration into host chromosomes. Its mechanism involves binding to the enzyme-DNA complex, inducing conformational changes that inhibit strand transfer. Structurally, the cyano group and aromatic rings enhance enzyme interaction. It is a crystalline solid with good aqueous solubility and metabolic stability, critical for antiretroviral therapy efficacy.