abacavir-lamivudine-zidovudine

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Trade Name(s): Abacavir/Lamivudine/Zidovudine; Trizivir
Group 2: Non-Antineoplastic Hazardous AHFS Class: HIV Nucleoside and Nucleotide Reverse Transcriptase Inhibitors
Formweb: abacavir-lamivudine-zidovudine
Info Links: Chemotherapy Extravasation Policy
Mechanism of Action:

Abacavir: Abacavir is a carbocyclic synthetic nucleoside analogue and an antiviral agent. 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. Viral DNA growth is terminated because the incorporated nucleotide lacks a 3'-OH group, which is needed to form the 5′ to 3′ phosphodiester linkage essential for DNA chain elongation.
Reference: Drug Bank

Lamivudine: Lamivudine is a synthetic nucleoside analogue and is phosphorylated intracellularly to its active 5'-triphosphate metabolite, lamivudine triphosphate (L-TP). This nucleoside analogue is incorporated into viral DNA by HIV reverse transcriptase and HBV polymerase, resulting in DNA chain termination.
Reference: Drug Bank

Zidovudine: Zidovudine, a structural analog of thymidine, is a prodrug that must be phosphorylated to its active 5′-triphosphate metabolite, zidovudine triphosphate (ZDV-TP). It inhibits the activity of HIV-1 reverse transcriptase (RT) via DNA chain termination after incorporation of the nucleotide analogue. It competes with the natural substrate dGTP and incorporates itself into viral DNA. It is also a weak inhibitor of cellular DNA polymerase α and γ.
Reference: Drug Bank

Exposure Risk:

abacavir:

  • Suspected of causing genetic defects.
  • Suspected of causing cancer.
  • Suspected of damaging fertility or the unborn child.
  • Causes serious eye irritation.
  • May cause an allergic skin reaction.

Reference: SDS - Cayman Chemical

lamivudine:

  • Suspected of damaging fertility or the unborn child.

Reference: SDS - Cayman Chemical

zidovudine:

  • Suspected of causing genetic defects.
  • May cause cancer.
  • Causes damage to organs through prolonged or repeated exposure.

Reference: SDS - Cayman Chemical

Safety Data Sheet(s):
Supplemental Information:

abacavir:
NIOSH 2016 & 2020: Malignant tumors observed in male and female mice and rats; Genotoxic in vivo micro-nucleus test.

zidovudine:
NIOSH 2016 & 2020: IARC Group 2B

Approved on November 22, 2024