Bexirestrant is a selective estrogen receptor degrader (SERD) which is being evaluated for the treatment of breast cancer. This orally bioavailable compound has demonstrated potent activity against both wild-type and mutant forms of the estrogen receptor (ER), addressing a critical need in overcoming resistance to current endocrine therapies.[1]

Bexirestrant
Clinical data
Other namesSCO-120
Identifiers
  • (2S)-3-(3,5-difluorophenyl)-2-[4-[(E)-3-[3-(fluoromethyl)azetidin-1-yl]prop-1-enyl]phenyl]-4-methyl-2H-chromen-7-ol
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC29H26F3NO2
Molar mass477.527 g·mol−1
3D model (JSmol)
  • CC1=C([C@@H](OC2=C1C=CC(=C2)O)C3=CC=C(C=C3)/C=C/CN4CC(C4)CF)C5=CC(=CC(=C5)F)F
  • InChI=InChI=1S/C29H26F3NO2/c1-18-26-9-8-25(34)14-27(26)35-29(28(18)22-11-23(31)13-24(32)12-22)21-6-4-19(5-7-21)3-2-10-33-16-20(15-30)17-33/h2-9,11-14,20,29,34H,10,15-17H2,1H3/b3-2+/t29-/m0/s1
  • Key:DVZLOPUYTKPWHJ-MPWQXXDYSA-N

It is structurally characterized by an E-alkene linked to an azetidine core.

References

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  1. ^ Min J, Liu X, Peng R, Chen CC, Wang W, Guo RT (February 2024). "New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives". Acta Materia Medica. 3 (1): 57–71. doi:10.15212/amm-2024-0006. PMC 11450757. PMID 39373009.