What is relugolix, and how does it function as a therapeutic agent in uterine diseases?

Label:chem

Topic
Relugolix is a novel, orally active, non-peptidic gonadotropin-releasing hormone (GnRH) receptor antagonist that suppresses luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion, thereby lowering ovarian estrogen and progesterone production. It is approved for the treatment of heavy menstrual bleeding (HMB) associated with uterine fibroids (UFs) and pain associated with endometriosis.
Answer
Relugolix competitively binds to pituitary GnRH receptors, rapidly reducing LH and FSH and leading to a dose-dependent decline in serum estradiol and progesterone. This mechanism alleviates UF-related HMB and endometriosis-related pain without the initial “flare-up” seen with GnRH agonists.
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