Saridegib

Saridegib, also known as IPI-926, is an experimental drug candidate undergoing clinical trials for the treatment of various types of cancer, including hard-to-treat hematologic malignancies such as myelofibrosis and ligand-dependent tumors such as chondrosarcoma.[1] IPI-926 exhibits its pharmacological effect by inhibition of the G protein-coupled receptor smoothened, a component of the hedgehog signaling pathway.[2] Chemically, it is a semi-synthetic derivative of the alkaloid cyclopamine. The process begins with cyclopamine extracted from harvested Veratrum californicum which is taken through a series of alterations resulting in an analogue of the natural product cyclopamine, making IPI-926 the only compound in development/testing that is not fully synthetic.[2]

Saridegib
Names
IUPAC name
N-((2S,3R,3aS,3R,4aR,6S,6aR,6bS,7aR,12aS,12bS)-3,6,11,12b-tetramethyl-2,3a,3,4,4,4a,5,5,6,6,6a,6b,7,7a,7,8,10,12,12a,12b-icosahydro-1H,3H-spiro[furo[3,2-b]pyridine-2,9'-naphtho[2,1-a]azulen]-3'-yl)methanesulfonamide
Other names
saridegib
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
KEGG
UNII
Properties
C29H48N2O3S
Molar mass 504.77 g·mol−1
Pharmacology
Oral
Legal status
  • Investigational
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references

Saridegib is a member of a class of anti-cancer compounds known as hedgehog pathway inhibitors.

References

  1. "Pipeline: IPI-926". Infinity Pharmaceuticals. Archived from the original on 2012-01-19.CS1 maint: unfit URL (link)
  2. Tremblay, MR; Lescarbeau, A; Grogan, MJ; Tan, E; Lin, G; Austad, BC; Yu, LC; Behnke, ML; et al. (2009). "Discovery of a potent and orally active hedgehog pathway antagonist (IPI-926)". Journal of Medicinal Chemistry. 52 (14): 4400–18. doi:10.1021/jm900305z. PMID 19522463.
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