维拉立生

化合物

维拉立生INN:vilaprisan;开发代号:BAY-1002670)是一种合成的类固醇选择性孕酮受体调节剂英语Selective progesterone receptor modulator,由拜耳医药保健制药公司正在开发,用于治疗子宫内膜异位症子宫肌瘤[1][2][3]它是一种有效且高度选择性英语Binding selectivity孕酮受体部分激动剂[4][2][3]截至2017年 (2017-Missing required parameter 1=month!),该药物正处于上述适应症的II期临床试验中。[1]

维拉立生
臨床資料
其他名稱BAY-1002670、17β-羟基-11β-[4-(甲磺酰基)苯基]-17α-(1,1,2,2,2-五氟乙基)雌-4,9-二烯-3-酮
给药途径口服
藥物類別英语Drug class选择性孕酮受体调节剂英语Selective progesterone receptor modulator
识别信息
  • (8S,11R,13S,14S,17S)-17-Hydroxy-13-methyl-11-(4-methylsulfonylphenyl)-17-(1,1,2,2,2-pentafluoroethyl)-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one
CAS号1262108-14-4
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C27H29F5O4S
摩尔质量544.58 g·mol−1
3D模型(JSmol英语JSmol
  • C[C@]12C[C@@H](C3=C4CCC(=O)C=C4CC[C@H]3[C@@H]1CC[C@]2(C(C(F)(F)F)(F)F)O)C5=CC=C(C=C5)S(=O)(=O)C
  • InChI=1S/C27H29F5O4S/c1-24-14-21(15-3-7-18(8-4-15)37(2,35)36)23-19-10-6-17(33)13-16(19)5-9-20(23)22(24)11-12-25(24,34)26(28,29)27(30,31)32/h3-4,7-8,13,20-22,34H,5-6,9-12,14H2,1-2H3/t20-,21+,22-,24-,25-/m0/s1
  • Key:JUFWQQVHQFDUOD-ANRPBIDPSA-N

参考资料

  1. ^ 1.0 1.1 Vilaprisan - Bayer HealthCare Pharmaceuticals - AdisInsight. [2024-04-26]. (原始内容存档于2024-05-01). 
  2. ^ 2.0 2.1 Whitaker LH, Williams AR, Critchley HO. Selective progesterone receptor modulators. Curr. Opin. Obstet. Gynecol. 2014, 26 (4): 237–42. PMID 24950125. S2CID 37474964. doi:10.1097/GCO.0000000000000082. 
  3. ^ 3.0 3.1 Pluchino N, Freschi L, Wenger JM, Streuli I. Innovations in classical hormonal targets for endometriosis. Expert Rev Clin Pharmacol. 2016, 9 (2): 317–27. PMID 26645363. S2CID 8624056. doi:10.1586/17512433.2016.1129895. 
  4. ^ Schütt B, Kaiser A, Schultze-Mosgau MH, Seitz C, Bell D, Koch M, Rohde B. Pharmacodynamics and safety of the novel selective progesterone receptor modulator vilaprisan: a double-blind, randomized, placebo-controlled phase 1 trial in healthy women. Hum. Reprod. 2016, 31 (8): 1703–12. PMID 27288475. doi:10.1093/humrep/dew140 . 

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