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fiacitabine
- Development stage
- Phase 2
- Lead developer
- Wellcome
- 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
- Intravenous, Oral
01
Overview
Fiacitabine is a synthetic nucleoside analogue structurally related to cytarabine and gemcitabine. It was developed as an antiviral agent with activity against herpesviruses and other DNA viruses. Fiacitabine acts by inhibiting viral DNA polymerase after being phosphorylated intracellularly to its active triphosphate form, thereby interfering with viral DNA synthesis. Despite promising preclinical results, clinical development was discontinued due to toxicity concerns (notably nephrotoxicity) and lack of sufficient efficacy in human trials.
- Other names
- 1-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)cytosineFNCarabinofuranosyl cytosine fluorinated analog
02
Targets
DNA polymerase family
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