Zovegalisib

Zovegalisib
Clinical data
Other namesRLY-2608
Identifiers
  • N-[(3R)-3-(2-chloro-5-fluorophenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxo-2,3-dihydroisoindol-4-yl]-3-fluoro-5-(trifluoromethyl)benzamide
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
PDB ligand
Chemical and physical data
FormulaC29H14ClF5N6O2
Molar mass608.91 g·mol−1
3D model (JSmol)
  • C1=CC(=C(C=C1F)[C@H]2C3=C(C=C(C=C3NC(=O)C4=CC(=CC(=C4)F)C(F)(F)F)C5=C(N6C(=NC=N6)C=C5)C#N)C(=O)N2)Cl
  • InChI=InChI=1S/C29H14ClF5N6O2/c30-21-3-1-16(31)10-19(21)26-25-20(28(43)40-26)7-13(18-2-4-24-37-12-38-41(24)23(18)11-36)8-22(25)39-27(42)14-5-15(29(33,34)35)9-17(32)6-14/h1-10,12,26H,(H,39,42)(H,40,43)/t26-/m0/s1
  • Key:VYWRYBZVVSPTQN-SANMLTNESA-N

Zovegalisib is an investigational new drug that is being evaluated by Relay Therapeutics for the treatment of HER2 negative breast cancer.[1] It is a phosphatidylinositol 3 kinase alpha inhibitor.[1][2][3]

References

  1. 1 2 "Zovegalisib". AdisInsight. Springer Nature Switzerland AG. Retrieved 5 July 2026.
  2. ↑ Varkaris A, Pazolli E, Gunaydin H, Wang Q, Pierce L, Boezio AA, et al. (February 2024). "Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia". Cancer Discovery. 14 (2): 240–257. doi:10.1158/2159-8290.CD-23-0944. PMC 10850943. PMID 37916956.
  3. ↑ Liu X, Chen Y, Han W, Chen Y, Feng W, Zhou Q, et al. (January 2026). "Structural Insights into the Development of Inhibitors Against Cancer-Specific Mutations of PI3Kα". Annual Review of Pharmacology and Toxicology. 66 (1): 465–485. doi:10.1146/annurev-pharmtox-082924-022724. PMID 40829787.
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