Olema Oncology is advancing the development of Palazestrant (OP-1250) in metastatic breast cancer in 2024. Palazestrant is an oral complete ER antagonist (CERAN) and selective ER degrader (SERD). It potently binds and completely blocks transcriptional activity of both wild-type and ESR1-mutant ER with favorable tolerability and anti-tumor activity.
Palazestrant is under clinical development both in combination with Novartis' CDK4/6 inhibitor Kisqali (Ribociclib) as a first-line therapy for advanced estrogen receptor-positive, HER2-negative breast cancer, and as a monotherapy compared to standard of care treatment in second- and third-line advanced or metastatic ER-positive, HER2-negative breast cancer.