Description
Abacavir-d
4 is intended for use as an internal standard for the quantification of abacavir by GC- or LC-MS. Abacavir is a nucleoside analog and an inhibitor of HIV-1 reverse transcriptase (K
i = 2.1 μM for the wild-type enzyme). It inhibits replication of a variety of HIV-1 and HIV-2 strains, including strains resistant to 3''-azido-3''-deoxythymidine (zidovudine; ) or 2'',3''-dideoxyinosine (didanosine; ), in HeLa cells stably expressing CD4 (IC
50s = 5.8-21 μM). Abacavir inhibits replication of eight HIV-1 clinical isolates in phytohemagglutinin-stimulated isolated human peripheral blood lymphocytes with a mean IC
50 value of 0.26 μM. It inhibits hepatitis B virus (HBV) DNA synthesis in HepG2 cells (IC
50 = 7 μM) and is also active against human cytomegalovirus (CMV) strain AD169 and the Petaluma strain of feline immunodeficiency virus (FIV) in plaque reduction assays (IC
50s = 32 and 0.4 μM, respectively). Formulations containing abacavir have been used in the treatment of HIV infection.
Uses
Abacavir-d4 is deuterium labeled Abacavir (A104990). Abacavir is a carbocyclic 2''-deoxyguanosine nucleoside reverse transcriptase inhibitor and an anti-HIV drug used to treat HIV infection (1). Intracellular enzymes convert Abacavir to its active form, carbovir-triphosphate (CBV-TP), which then selectively inhibits HIV reverse transcriptase by incorporating into viral DNA (2). Abacavir is metabolized in the liver by uridine diphosphate glucuronyltransferase and alcohol dehydrogenase resulting in inactive glucuronide and carboxylate metabolites, respectively.
