Giredestrant

Giredestrant (GDC-9545), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity[1].

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

ER

Giredestrant (GDC-9545) is a novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes. The highly potent in vivo efficacy of Giredestrant likely arises due to the particular combination of high binding potency, full suppression of ER signaling, and an improved DMPK profile[1].

[1]. C Metcalfe, et al. Abstract P5-04-07: GDC-9545: A novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes