维拉立生
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 选择性孕酮受体调节剂 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 (EPA ) 化学信息 化学式 C 27 H 29 F 5 O 4 S 摩尔质量 544.58 g·mol−1 3D模型(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
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 ,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 和子宫肌瘤 。[1] [2] [3] 它是一种有效 且高度选择性 的孕酮受体 部分激动剂 。[4] [2] [3] 截至2017年 (2017-Missing required parameter 1=month ! ) [update] ,该药物正处于上述适应症的II期临床试验中。[1]
参考资料
^ 1.0 1.1 Vilaprisan - Bayer HealthCare Pharmaceuticals - AdisInsight .
^ 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 .
^ 3.0 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 .
^ 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 .
外部链接
PR
受體致活劑
Mixed (SPRMs )
Apigenin
Asoprisnil
Asoprisnil ecamate
Guggulsterone
山柰酚
J1042
LG-120838
Naringenin
PRA-910
丁香酸
Telapristone
受體拮抗劑: 美服培酮
Org-31710
Org-33628
Ulipristal acetate
ZK-137316
Antagonists
3α-Hydroxytibolone
3β-Hydroxytibolone
阿来司酮
利洛司酮
洛那立生
奥那司酮
托立司酮
丙戊酸
维拉立生
扎诺特隆
ZM-150271
ZM-172406
mPRs (PAQRs )
受體致活劑
5α-Dihydroprogesterone
5β-Dihydroprogesterone
11-脱氧皮质酮
17α-Hydroxyprogesterone
17α,21-Dihydroxyprogesterone
Allopregnanolone
美服培酮
孕烯醇酮
孕酮
Antagonists
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