GDC-0810 + lhrh agonist

**GDC-0810 + lhrh agonist** is a combination therapy consisting of GDC-0810 (ARN-810), a novel, non-steroidal, orally bioavailable selective estrogen receptor degrader (SERD), and a luteinizing hormone-releasing hormone (LHRH) agonist. In phase Ib clinical cohorts, this combination targeted patients with estrogen receptor-positive (ER+), HER2-negative, locally advanced or metastatic breast cancer. GDC-0810 inhibits ligand-dependent and ligand-independent estrogen receptor-mediated signaling, leading to downregulation and degradation of the estrogen receptor. LHRH agonists suppress ovarian estrogen production by continuous stimulation of the pituitary receptors, leading to downregulation and suppression of gonadotropin release, effectively inducing chemical menopause, which is especially relevant in premenopausal or perimenopausal women. The combination is designed for endocrine manipulation in advanced breast cancers dependent on estrogen signaling. Typical side effects observed include diarrhea, nausea, fatigue, vomiting, and constipation. Dose-finding and pharmacokinetics established 600 mg GDC-0810 (oral, daily with food) as the recommended Phase 2 dose; LHRH agonists were administered by injection every 28 days.[3][5][7]

Other names

GDC-0810 + luteinizing hormone-releasing hormone agonistGDC-0810 + LHRH agonist