Giredestrant
Giredestrant (also known as GDC-9545, RG6171, or RO7197597) is an investigational oral selective estrogen receptor degrader (SERD) developed by Genentech, a member of the Roche Group, for the treatment of estrogen receptor-positive (ER+), HER2-negative advanced breast cancer, as well as endometrial cancer, ovarian cancer, and other solid tumors. It is a potent, nonsteroidal compound that antagonizes estrogen effects by competitively binding to both wild-type and mutant estrogen receptors with nanomolar potency. Giredestrant works by inducing an inactive conformation of the estrogen receptor ligand-binding domain and promoting proteasome-mediated degradation of the receptor protein. As of May 2025, giredestrant is in clinical trials and has received Fast Track designation from the Food and Drug Administration (FDA) for ER+, HER2-negative second- and third-line metastatic breast cancer. Mechanism of action Giredestrant is a nonsteroidal SERD that binds the estrogen receptor (E ...
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