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zalcitabine
- Development stage
- Phase 3
- Lead developer
- Roche
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Zalcitabine is a synthetic nucleoside analogue of deoxycytidine and belongs to the class of nucleoside reverse transcriptase inhibitors (NRTIs). It was developed as an antiretroviral agent for the treatment of HIV-1 infection. Zalcitabine works by being phosphorylated within cells to its active metabolite, dideoxycytidine 5'-triphosphate (ddCTP), which inhibits HIV reverse transcriptase by competing with natural substrates and incorporating into viral DNA. This incorporation terminates DNA chain elongation due to the absence of a 3'-hydroxyl group, thereby blocking viral replication. Zalcitabine was used in combination with other antiretrovirals but has been discontinued due to the availability of newer therapies and concerns about side effects such as peripheral neuropathy. The drug was originally marketed under the brand name Hivid[2][6][7][8].
- Brand names
- Hivid
- Other names
- ddC2',3'-dideoxycytidine
02
Targets
Human immunodeficiency virus type 1 reverse transcriptasePOLG (Mitochondrial DNA polymerase gamma)
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