Dolutegravir

Definition

An orally bioavailable integrase strand-transfer inhibitor (INSTI), with activity against human immunodeficiency virus type 1 (HIV-1) infection. Upon oral administration, dolutegravir binds to the active site of integrase, an HIV enzyme that catalyzes the transfer of viral genetic material into human chromosomes. This prevents integrase from binding to retroviral deoxyribonucleic acid (DNA), and blocks the strand transfer step, which is essential for the HIV replication cycle. This prevents HIV-1 replication.

Also known as 2H-Pyrido(1',2':4,5)pyrazino(2,1-b)(1,3)oxazine-9-carboxamide, N-((2,4-difluorophenyl)methyl)-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-, (4R,12aS), DOLUTEGRAVIR, DTG, GSK 1349572, GSK-1349572 — per NCIT

Also identified as

• ATC J05AJ per NCIT
• ATC J05AR per NCIT
• NCIT NCIT:C121543 per NCIT

Indications