Abacavir lamivudine
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Overview
Abacavir/lamivudine (INNs) is a combination drug for the treatment of HIV infection. It is marketed as Kivexa in most countries except for the United States, where it is branded as Epzicom.[1] It is a fixed dose combination of lamivudine (3TC, Epivir) and abacavir (ABC, Ziagen).
Lamivudine and abacavir are both nucleoside reverse transcriptase inhibitors (NRTI).
It was approved by the FDA on August 2, 2004. It is marketed by ViiV Healthcare.
Category
Antiretroviral
US Brand Names
EPZICOM®
FDA Package Insert
Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Overdosage | Clinical Studies | Dosage and Administration | How Supplied | Labels and Packages
Mechanism of Action
Abacavir
Abacavir is a carbocyclic synthetic nucleoside analogue. Abacavir is converted by cellular enzymes to the active metabolite, carbovir triphosphate (CBV-TP), an analogue of deoxyguanosine-5′-triphosphate (dGTP). CBV-TP inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA. The lack of a 3′-OH group in the incorporated nucleotide analogue prevents the formation of the 5′ to 3′ phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. CBV-TP is a weak inhibitor of cellular DNA polymerases α, β, and γ.
Lamivudine
Lamivudine is a synthetic nucleoside analogue. Intracellularly lamivudine is phosphorylated to its active 5′-triphosphate metabolite, lamivudine triphosphate (3TC-TP). The principal mode of action of 3TC-TP is inhibition of RT via DNA chain termination after incorporation of the nucleotide analogue. CBV-TP and 3TC-TP are weak inhibitors of cellular DNA polymerases α, β, and γ.