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Vilaprisan Other names BAY-1002670; 17β-Hydroxy-11β-[4-(methylsulfonyl)phenyl]-17α-(1,1,2,2,2-pentafluoroethyl)estra-4,9-dien-3-one Routes of administration By mouth Drug class Selective progesterone receptor modulator
(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 Number PubChem CID ChemSpider UNII CompTox Dashboard (EPA ) Formula C 27 H 29 F 5 O 4 S Molar mass 544.58 g·mol−1 3D model (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
Vilaprisan (INN Tooltip International Nonproprietary Name , USAN Tooltip United States Adopted Name ) (developmental code name BAY-1002670 ) is a synthetic and steroidal selective progesterone receptor modulator (SPRM) which is under development by Bayer HealthCare Pharmaceuticals for the treatment of endometriosis and uterine fibroids .[ 1] [ 2] [ 3] It is a potent and highly selective partial agonist of the progesterone receptor (PR).[ 4] [ 2] [ 3] As of 2017, the drug is in phase II clinical trials for the aforementioned indications.[ 1]
See also
References
^ a b http://adisinsight.springer.com/drugs/800033040
^ a b Whitaker LH, Williams AR, Critchley HO (2014). "Selective progesterone receptor modulators". Curr. Opin. Obstet. Gynecol . 26 (4): 237–42. doi :10.1097/GCO.0000000000000082 . PMID 24950125 .
^ a b Pluchino N, Freschi L, Wenger JM, Streuli I (2016). "Innovations in classical hormonal targets for endometriosis". Expert Rev Clin Pharmacol . 9 (2): 317–27. doi :10.1586/17512433.2016.1129895 . PMID 26645363 .
^ Schütt B, Kaiser A, Schultze-Mosgau MH, Seitz C, Bell D, Koch M, Rohde B (2016). "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 . 31 (8): 1703–12. doi :10.1093/humrep/dew140 . PMID 27288475 .
External links
PR Tooltip Progesterone receptor
Agonists
Testosterone derivatives: Progestins: 6,6-Difluoronorethisterone
6,6-Difluoronorethisterone acetate
17α-Allyl-19-nortestosterone
Allylestrenol
Altrenogest
Chloroethynylnorgestrel
Cingestol
Danazol
Desogestrel
Dienogest
Ethinylandrostenediol
Ethisterone
Ethynerone
Etonogestrel
Etynodiol
Etynodiol diacetate
Gestodene
Gestrinone
Levonorgestrel
Levonorgestrel esters (e.g., levonorgestrel butanoate )
Lynestrenol
Lynestrenol phenylpropionate
Metynodiol
Metynodiol diacetate
Norelgestromin
Norethisterone (norethindrone)
Norethisterone esters (e.g., norethisterone acetate , norethisterone enanthate )
Noretynodrel
Norgesterone
Norgestimate
Norgestrel
Norgestrienone
Norvinisterone
Oxendolone
Quingestanol
Quingestanol acetate
Tibolone
Tigestol
Tosagestin ; Anabolic–androgenic steroids: 11β-Methyl-19-nortestosterone
11β-Methyl-19-nortestosterone dodecylcarbonate
19-Nor-5-androstenediol
19-Nor-5-androstenedione
19-Nordehydroepiandrosterone
Bolandiol
Bolandiol dipropionate
Bolandione
Dimethisterone
Dienedione
Dienolone
Dimethandrolone
Dimethandrolone buciclate
Dimethandrolone dodecylcarbonate
Dimethandrolone undecanoate
Dimethyldienolone
Dimethyltrienolone
Ethyldienolone
Ethylestrenol (ethylnandrol)
Methyldienolone
Metribolone (R-1881)
Methoxydienone (methoxygonadiene)
Mibolerone
Nandrolone
Nandrolone esters (e.g., nandrolone decanoate , nandrolone phenylpropionate )
Norethandrolone
Normethandrone (methylestrenolone, normethandrolone, normethisterone)
RU-2309
Tetrahydrogestrinone
Trenbolone (trienolone)
Trenbolone esters (e.g., trenbolone acetate , trenbolone enanthate )
Trendione
Trestolone
Trestolone acetate
Mixed (SPRMs Tooltip Selective progesterone receptor modulators ) Antagonists
mPR Tooltip Membrane progesterone receptor (PAQR Tooltip Progestin and adipoQ receptor )