Indole is a compound of pyrrole and benzene in parallel, also known as benzopyrrole. There are two combinations of pyrrole and benzene, called indole and isoindole, respectively. Many derivatives of indole have physiological and pharmacological activities, and can synthesize vasodilators, antihistamines, antipyretic analgesics, etc. in medicine, so indole is also a very important heterocyclic compound.
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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.