PubChem CID 56941241 UNII 9MM2R1A06R | CAS Number 1365888-06-7 ChemSpider 35308225 Molar mass 446.9006 g/mol | |
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Synonyms GDC-0810, ARN-810, RG-6046, RO-7056118 | ||
Brilanestrant (INN) (developmental code names GDC-0810, ARN-810, RG-6046, RO-7056118) is a non-steroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) that was discovered by Aragon Pharmaceuticals and is under development by Genentech for the treatment of locally advanced or metastatic estrogen receptor (ER)-positive breast cancer. As of September 2016, it is in phase II clinical trials for this indication.
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.
Brilanestrant is a structural analogue of etacstil, an earlier combined SERM and SERD that was abandoned in 2001 for commercial reasons.