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Orelzagol is an orally active, small-molecule gonadotropin-releasing hormone (GnRH) receptor antagonist developed by Qilu Pharmaceutical. It is primarily being investigated for the management of moderate to severe pain associated with endometriosis. By competitively binding to GnRH receptors in the pituitary gland, orelzagol suppresses the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn leads to a dose-dependent reduction in ovarian estrogen production. This mechanism creates a hypoestrogenic environment that inhibits the growth of endometrial tissue and alleviates associated pelvic pain. As of 2024, orelzagol is undergoing Phase 3 clinical evaluation in China.
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