中文名称 | 噁拉戈利 |
---|---|
英文名称 | Elagolix (NBI-56418) |
CAS号 | 834153-87-6 |
分子式 | C32H30F5N3O5 |
分子量 | 631.59 |
外观 | White to off-white powder |
储存条件 | Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years). |
Elagolix (formerly NBI56418; ABT620; NBI-56418; ABT-620; trade name: Orilissa) is a potent, specific, orally bioavailable, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) used for pain management. It inhibits GnRHR with a Kd of 54 pM. Elagolix was given FDA approval on July 23, 2018, to treat endometriosis-related moderate to severe pain. A short-acting GnRH antagonist, elagolix suppresses ovarian estrogen production in a dose-dependent manner, resulting in partial suppression at lower doses and complete suppression at higher doses. Because Elagolix is non-peptide and readily absorbed through the mouth, it is considered the leader of a new class of GnRH inhibitors known as second-generation inhibitors.
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