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fosciclopirox
- Development stage
- Phase 2
- Lead developer
- CicloMed
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
- Administration
- Intravenous, Intravesical
01
Overview
Fosciclopirox is a phosphoryloxymethyl ester-based prodrug of ciclopirox (CPX), a synthetic broad-spectrum antifungal agent with antibacterial, anti-inflammatory, and potential antineoplastic activities[1][3]. Developed as a water-soluble compound for parenteral administration, fosciclopirox is rapidly metabolized in the blood to its active form, ciclopirox. The drug selectively delivers ciclopirox to the urinary tract and has shown significant anticancer activity in preclinical models of both non-muscle invasive and muscle-invasive bladder cancer[3][4][7]. Mechanistically, fosciclopirox acts as an inhibitor of the gamma-secretase complex—specifically binding to Presenilin 1 and Nicastrin proteins—thereby suppressing Notch signaling pathways implicated in cancer progression[3][4][5][8]. It also inhibits Wnt signaling pathways. Fosciclopirox is currently being evaluated in Phase 1/2 clinical trials for bladder cancer and acute myeloid leukemia (AML)[5][7].
- Other names
- CPX-POMciclopirox prodrug
02
Targets
GSEC (Gamma-Secretase Complex)
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