Bictegravir is a monocarboxylic acid amide formed by the formal condensation of the carboxy group of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxylic acid with the amino group of 2,4,6-trifluorobenzylamine. It is a second-generation integrase strand transfer inhibitor (INSTI) used (as its sodium salt) for the treatment of HIV-1. It functions as a HIV-1 integrase inhibitor and is classified as a monocarboxylic acid amide, a secondary carboxamide, a trifluorobenzene, and an organic heterotetracyclic compound. It is also the conjugate acid of bictegravir(1-).