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safingol
- Development stage
- Phase 1
- Lead developer
- Research Triangle Park Laboratories
- Modality
- Small Molecules
- Administration
- Intravenous, Topical
01
Overview
Safingol is a synthetic lyso-sphingolipid and an analogue of sphingosine that functions primarily as a protein kinase C (PKC) inhibitor and sphingosine kinase (SphK) inhibitor. It has demonstrated anticancer potential, particularly as a chemosensitizer that enhances the cytotoxic effects of various chemotherapeutic agents by promoting drug-induced apoptosis and autophagy. Safingol competitively inhibits several PKC isoforms (including PKCβ-I, PKCδ, and PKCε), as well as phosphoinositide 3-kinase (PI3k), thereby affecting key signaling pathways such as mTOR and MAPK/ERK. Its mechanism involves induction of necrotic cell death via reactive oxygen species generation and autophagy, rather than classic apoptosis. Safingol has been evaluated in clinical trials for cancer in combination with other chemotherapies but has limited single-agent activity[1][3][4][5][6][7].
- Brand names
- KynacKynacyte
- Other names
- L-threo-dihydrosphingosineL-threo-sphinganinesafingol
02
Targets
PRKCE (Protein Kinase C epsilon)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)PRKCB (Protein kinase C beta)SPHK1 (Sphingosine kinase 1)PRKCD (Protein kinase C delta)
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