molecules of the month


selective ER degrader (SERD) + full antagonist

oral (30 mg QD), Ph. III for ER+, HER2- BC

from profiling >4k cmpds for desired MoA

Journal of Medicinal Chemistry

Genentech, San Francisco, US

Chemical structure of Giredestrant
1 min read

The Genentech next generation oral SERD (selective estrogen receptor degrader) and full antagonist, giredestrant (GDC-9545), is a potential best-in-class Ph. III candidate for ER+, HER2- breast cancer (NCT04546009). It is the third SERD clinical candidate from Genentech (after GDC-0810 and GDC-0927) and a number of oral SERDs have previously been highlighted here (including SAR439659, AZD9833, GNE-149) The oral, once-daily molecule has been well-tolerated at doses up to 250 mg and a standardized 30 mg dose has been selected for development. Interim analysis and updated data from trials NCT03916744 and NCT03332797 show promising activity including in the presence of ESR1 mutations. Hormone therapy is a mainstay of treatment for breast cancer, but side effects have a significant quality of life impact and affect treatment adherence. A well-tolerated, easily combinable, and effective ER degrader could…

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