From Wikipedia, the free encyclopedia
Chemical compound
Vilaprisan
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Other names | BAY-1002670; 17β-Hydroxy-11β-[4-(methylsulfonyl)phenyl]-17α-(1,1,2,2,2-pentafluoroethyl)estra-4,9-dien-3-one |
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Routes of administration |
By mouth |
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Drug class |
Selective progesterone receptor modulator |
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(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
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CAS Number | |
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PubChem
CID | |
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ChemSpider | |
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UNII | |
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KEGG | |
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Formula | C27H29F5O4S |
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Molar mass | 544.58 g·mol−1 |
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3D model (
JSmol) | |
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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
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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
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Vilaprisan (
INNTooltip International Nonproprietary Name,
USANTooltip 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
"Vilaprisan - Bayer HealthCare Pharmaceuticals - AdisInsight".
- ^
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.
S2CID
37474964.
- ^
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.
S2CID
8624056.
-
^ 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
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PRTooltip Progesterone receptor | Agonists |
- Testosterone derivatives: Progestins:
6,6-Difluoronorethisterone
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6,6-Difluoronorethisterone acetate
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17α-Allyl-19-nortestosterone
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Allylestrenol
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Altrenogest
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Chloroethynylnorgestrel
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Cingestol
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Danazol
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Desogestrel
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Dienogest
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Ethinylandrostenediol
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Ethisterone
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Ethynerone
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Etonogestrel
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Etynodiol
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Etynodiol diacetate
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Gestodene
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Gestrinone
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Levonorgestrel
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Levonorgestrel esters (e.g.,
levonorgestrel butanoate)
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Lynestrenol
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Lynestrenol phenylpropionate
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Metynodiol
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Metynodiol diacetate
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Norelgestromin
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Norethisterone (norethindrone)
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Norethisterone esters (e.g.,
norethisterone acetate,
norethisterone enanthate)
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Noretynodrel
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Norgesterone
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Norgestimate
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Norgestrel
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Norgestrienone
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Norvinisterone
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Oxendolone
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Quingestanol
-
Quingestanol acetate
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Tibolone
-
Tigestol
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Tosagestin; Anabolic–androgenic steroids:
11β-Methyl-19-nortestosterone
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11β-Methyl-19-nortestosterone dodecylcarbonate
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19-Nor-5-androstenediol
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19-Nor-5-androstenedione
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19-Nordehydroepiandrosterone
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Bolandiol
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Bolandiol dipropionate
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Bolandione
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Dimethisterone
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Dienedione
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Dienolone
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Dimethandrolone
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Dimethandrolone buciclate
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Dimethandrolone dodecylcarbonate
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Dimethandrolone undecanoate
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Dimethyldienolone
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Dimethyltrienolone
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Ethyldienolone
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Ethylestrenol (ethylnandrol)
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Methyldienolone
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Metribolone (R-1881)
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Methoxydienone (methoxygonadiene)
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Mibolerone
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Nandrolone
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Nandrolone esters (e.g.,
nandrolone decanoate,
nandrolone phenylpropionate)
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Norethandrolone
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Normethandrone (methylestrenolone, normethandrolone, normethisterone)
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RU-2309
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Tetrahydrogestrinone
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Trenbolone (trienolone)
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Trenbolone esters (e.g.,
trenbolone acetate,
trenbolone enanthate)
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Trendione
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Trestolone
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Trestolone acetate
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Mixed (
SPRMsTooltip Selective progesterone receptor modulators) | |
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Antagonists | |
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mPRTooltip Membrane progesterone receptor (
PAQRTooltip Progestin and adipoQ receptor) | |
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