Elagolix Soidum (NBI-56418, ABT-620) 是一种有效的、选择性的、具有口服活性的促性腺激素释放激素受体GnRHR非肽段拮抗剂,Kd值为54 pM。浓度为10 μM时,对离子通道、酶和转运体没有显著的活性作用(inhibition <50%)。
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Overview
Elagolix Sodium is a small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist. Its molecular formula is C20H19F4N5NaO4 and CAS number is 1268075-96-2. The core synthesis involves multi-step organic coupling and salt formation.
Application
- Treatment of moderate to severe pain associated with endometriosis.
- Management of heavy menstrual bleeding in adult women with uterine leiomyomas.
- Pharmaceutical intermediate for controlled-release oral formulations.
Precautions
Strictly monitor bone mineral density during prolonged therapy. Avoid use in patients with severe hepatic impairment. Store in sealed containers at 2-8°C protected from light and moisture.