giredestrant

Giredestrant is a potent, orally bioavailable, nonsteroidal selective estrogen receptor degrader (SERD) that antagonizes the effects of estrogens by competitively binding to the ligand-binding domain of both wild-type and mutant estrogen receptors (ER), including those with ESR1 mutations. This binding induces a conformational change in the ER that promotes its proteasome-mediated degradation, thereby reducing ER protein levels and inhibiting ER-mediated signaling. Giredestrant has demonstrated preclinical and clinical activity in hormone receptor-positive (HR+), HER2-negative advanced breast cancer—including tumors resistant to other endocrine therapies—and is being investigated for use in other solid tumors such as rare ovarian and endometrial cancers. It is developed as an oral therapy with superior potency over earlier SERDs like fulvestrant[1][3][4][6][7].

Other names

1953133-47-5giredestrant [INN]giredestrant [USAN]