islatravir

Islatravir is an investigational small molecule antiretroviral drug developed for the treatment and prevention of HIV infection. It belongs to a novel class called nucleoside reverse transcriptase translocation inhibitors (NRTTIs). Islatravir acts as a deoxyadenosine analog and inhibits HIV reverse transcriptase through multiple mechanisms, including immediate chain termination by blocking translocation after incorporation into viral DNA, delayed chain termination via structural changes in the viral DNA chain, and misincorporation leading to nonextendable primers. Its active triphosphate form (islatravir-TP) has potent activity against both HIV-1 and HIV-2, including multidrug-resistant strains. Islatravir demonstrates high potency, a long intracellular half-life supporting infrequent dosing regimens (including monthly oral or implantable forms), and minimal risk of drug-drug interactions. The drug was placed on partial clinical hold in 2021 due to CD4 T cell declines but development has resumed at lower doses for treatment; PrEP studies have been discontinued[1][2][4][5][7].

Other names

4′-ethynyl-2-fluoro-2′-deoxyadenosine