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4'-Thio-fac
- Development stage
- Phase 2
- Lead developer
- Fujifilm
- 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, Intravenous (investigational)
01
Overview
4'-Thio-fac is a small molecule deoxycytidine analog with a unique thio and fluoro modification on the sugar moiety. It exhibits potent anti-proliferative and cytotoxic effects in vitro and in vivo against various solid tumors including colorectal, gastric, pancreatic (including gemcitabine-resistant), and ovarian cancers. The compound has demonstrated superior efficacy to standard chemotherapeutics such as gemcitabine, carboplatin, and paclitaxel in preclinical models. Its mechanism of action is believed to involve inhibition of DNA synthesis by incorporation into DNA as a nucleoside analog. It is under clinical investigation for advanced solid tumors and lymphomas[1][2][3].
- Other names
- 1-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl) cytosine4-amino-1-[(2R,3S,4S,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)thiolan-2-yl]pyrimidin-2-one
02
Targets
DNA polymerase family
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