- Source: Giredestrant
Giredestrant is an investigational oral selective estrogen receptor degrader (SERD) being developed for the treatment of estrogen receptor-positive (ER+) breast cancer. 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.
Research
In clinical trials, giredestrant has been evaluated in patients with ER+ breast cancer, including those with ESR1 mutations, both as a single agent and in combination with other therapies. Its orally bioavailable.