生物活性

• 描述Elagolix Sodium is a sodium form of Elagolix. Elagolix is a potent nonpeptide GnRHR (gonadotropin-releasing hormone receptor) antagonist and may be potential to the treatment of endometriosis. It exhibited affinity to hGnRHR with Ki value of 0.9nM and inhibited GnRH (6 nM) stimulated inositol phosphate (IP) production with IC50 value of 1.5nM. Oral administration of Elagolix at 30mg/kg suppressed luteinizing hormone in castrated male cynomolgus macaques^[3].

• 动物研究
  剂量	Monkey: 30 mg/kg[1] (p.o.) Beagle Dog: 10 mg/kg - 150 mg/kg[2] (p.o.) Rat: 300 mg/kg - 1200 mg/kg[2] (p.o.)
  给药途径	p.o.
  动物药代数据	Animal Rats[1] Dogs[1] Dose 10 mg/kg 50 mg/kg Administration i.v. or p.o. p.o. F 0.058 1 Vd 2.6 L/kg 0.92 L/kg T1/2 0.9 h 2.8 h Tmax 0.25 h 2 h CLp 33.3 ml/min/kg 14.5 ml/min/kg Cmax 338 ng/ml 13900 ng/ml AUC0→∞ 80700 ng/(ml·h) AUC 290 ng/(ml·h)

• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01403038	Folliculogenesis	Phase 1	Completed	-	United States, Colorado ... more >> Site Reference ID/Investigator# 50805 Colorado Springs, Colorado, United States, 80910 Site Reference ID/Investigator# 51270 Colorado Springs, Colorado, United States, 80917 Site Reference ID/Investigator# 50884 Denver, Colorado, United States, 80246 Site Reference ID/Investigator# 50404 Lonetree, Colorado, United States, 80124 United States, Florida Site Reference ID/Investigator# 50904 Miami, Florida, United States, 33126 Site Reference ID/Investigator# 50402 South Miami, Florida, United States, 33143 Site Reference ID/Investigator# 50808 Tampa, Florida, United States, 33606 United States, Illinois Site Reference ID/Investigator# 50807 Naperville, Illinois, United States, 60540 Site Reference ID/Investigator# 50804 Oak Brook, Illinois, United States, 60523 United States, North Carolina Site Reference ID/Investigator# 50762 Durham, North Carolina, United States, 27713 Site Reference ID/Investigator# 50403 Winston-Salem, North Carolina, United States, 27103 United States, Ohio Site Reference ID/Investigator# 50810 Cincinnati, Ohio, United States, 45267-0457 United States, Oregon Site Reference ID/Investigator# 50883 Portland, Oregon, United States, 97239 United States, Pennsylvania Site Reference ID/Investigator# 50803 Philadelphia, Pennsylvania, United States, 19104 Site Reference ID/Investigator# 51546 Philadelphia, Pennsylvania, United States, 19114 United States, Texas Site Reference ID/Investigator# 50806 San Antonio, Texas, United States, 78229 Site Reference ID/Investigator# 51342 San Antonio, Texas, United States, 78229 United States, Utah Site Reference ID/Investigator# 50811 Sandy, Utah, United States, 84070 United States, Virginia Site Reference ID/Investigator# 50902 Norfolk, Virginia, United States, 23507 United States, Washington Site Reference ID/Investigator# 50882 Seattle, Washington, United States, 98105 Puerto Rico Site Reference ID/Investigator# 53363 San Juan, Puerto Rico, 00935 Site Reference ID/Investigator# 53362 Santurce, Puerto Rico, 00910 Collapse <<
  NCT01441635	Heavy Uterine Bleeding ... more >> Uterine Fibroids Collapse <<	Phase 2	Completed	-	-
  NCT00797225	Endometriosis	Phase 2	Completed	-	-

• 更多
• 参考文献

• [1] Chen C, Wu D, et al. Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2008 Dec 11;51(23):7478-85.

  [2] ELAGOLIX SODIUM

  [3] Chen C, Wu D, Guo Z, Xie Q, Reinhart GJ, Madan A, Wen J, Chen T, Huang CQ, Chen M, Chen Y, Tucci FC, Rowbottom M, Pontillo J, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS. Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2008 Dec 11;51(23):7478-85. doi: 10.1021/jm8006454. PMID: 19006286.