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Abacavir


ACCESSION NB: DB01048 (APRD00216)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
Abacavir (ABC) is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS. [Wikipedia]

VOLUME OF DISTRIBUTION: 0.86 ± 0.15 L/kg

CATEGORIES:
Anti-HIV Agents Nucleoside and Nucleotide Reverse Transcriptase Inhibitors Reverse Transcriptase Inhibitors

ABSORPTION: Rapid and extensive after oral administration (83% bioavailability)

INDICATION:
For the treatment of HIV-1 infection, in combination with other antiretroviral agents.

PHARMACODYNAMICS:
Abacavir is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Abacavir is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated.

MECHANISM OF ACTION:
Abacavir is a carbocyclic synthetic nucleoside analogue. Intracellularly, abacavir is converted by cellular enzymes to the active metabolite carbovir triphosphate, an analogue of deoxyguanosine-5'-triphosphate (dGTP). Carbovir triphosphate inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA.

PROTEIN BINDING:
Moderate (approximately 50%)

METABOLISM:
Hepatic, by alcohol dehydrogenase and glucuronosyltransferase to a 5′-carboxylic acid metabolite and 5′-glucuronide metabolite, respectively. These metabolites have no antiviral activity. Abacavir is not significantly metabolized by cytochrome P450 enzymes.

TOXICITY:
Some myocardial degeneration has been noticed in rats and mice

AFECTED ORGANISMS:
Human Immunodeficiency Virus