Brilanestrant

Brilanestrant

Clinical data
Synonyms	GDC-0810, ARN-810, RG-6046, RO-7056118
Routes of administration	Oral
Identifiers
IUPAC name (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	1365888-06-7
PubChem CID	56941241
ChemSpider	35308225
UNII	9MM2R1A06R
Chemical and physical data
Formula	C26H20ClFN2O2
Molar mass	446.900603 g/mol
3D model (JSmol)	Interactive image
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 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

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.

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.

Similarly to tamoxifen, a SERM, brilanestrant shows some capacity to activate the ER in certain contexts and possesses weak estrogenic activity in the rat uterus, and unlike fulvestrant, which is currently the only SERD to have been marketed, brilanestrant is not a steroid and is orally bioavailable and does not need to be administered by intramuscular injection. Brilanestrant has been found to be active in tamoxifen- and fulvestrant-resistant in vitro models of human breast cancer.Side effects observed in clinical studies of brilanestrant thus far have included diarrhea, nausea, and fatigue of mostly mild-to-moderate severity.