Brilanestrant

Brilanestrant (INN) (developmental code names GDC-0810, ARN-810, RG-6046, RO-7056118) is a nonsteroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) that was discovered by Aragon Pharmaceuticals and was under development by Genentech for the treatment of locally advanced or metastatic estrogen receptor (ER)-positive breast cancer.

Brilanestrant
Clinical data
Other namesGDC-0810, ARN-810, RG-6046, RO-7056118
Routes of
administration
Oral
Identifiers
  • (2E)-3-{4-[(1E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl]phenyl}prop-2-enoic acid
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC26H20ClFN2O2
Molar mass446.91 g·mol−1
3D model (JSmol)
SMILES
  • CCC(=C(C1=CC=C(C=C1)C=CC(=O)O)C2=CC3=C(C=C2)NN=C3)C4=C(C=C(C=C4)F)Cl
  • InChI=1S/C26H20ClFN2O2/c1-2-21(22-10-9-20(28)14-23(22)27)26(18-8-11-24-19(13-18)15-29-30-24)17-6-3-16(4-7-17)5-12-25(31)32/h3-15H,2H2,1H3,(H,29,30)(H,31,32)/b12-5+,26-21+
  • Key:BURHGPHDEVGCEZ-KJGLQBJMSA-N

Development of brilanestrant was discontinued by Roche in April 2017. It reached phase II clinical trials for the treatment of breast cancer prior to the discontinuation of its development.

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