Giredestrant (GDC-9545) 是一种新型 ER 拮抗剂，结合了理想的机制和临床前 DMPK 属性。Giredestrant 的高效体内功效可能是由于其具有高 ER 结合力、ER 信号传导的完全抑制和改善的 DMPK 特征。 Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective 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