brilanestrant

Brilanestrant is an orally bioavailable, nonsteroidal small molecule that acts as a dual selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD). It was originally discovered by Aragon Pharmaceuticals and subsequently developed by Genentech (a subsidiary of Roche) for the treatment of estrogen receptor-positive (ER+) breast cancer. Brilanestrant works by binding to the estrogen receptor-alpha (ER-α) and inducing its degradation, which inhibits estrogen-mediated signaling and prevents the proliferation of ER-dependent tumor cells. Unlike fulvestrant, which is a steroidal SERD requiring intramuscular injection, brilanestrant was designed for convenient oral administration. Development of the agent progressed to Phase II clinical trials for advanced or metastatic breast cancer but was discontinued by Roche in April 2017.

Other names

brilanestrant