Telapristone Other names CDB-4124; Proellex; Progenta; 17β-(Acetyloxy)-11β-[4-(dimethylamino)phenyl]-17α-(2-methoxyacetyl)estra-4,9-dien-3-one Drug class Selective progesterone receptor modulator Legal status
[(8S ,11R ,13S ,14S ,17R )-11-[4-(Dimethylamino)phenyl]-17-(2-methoxyacetyl)-13-methyl-3-oxo-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a ]phenanthren-17-yl] acetate
CAS Number PubChem CID PubChem SID DrugBank ChemSpider UNII ChEMBL CompTox Dashboard (EPA ) Formula C 31 H 39 N O 5 Molar mass 505.655 g·mol−1 3D model (JSmol )
O=C5\C=C3/C(=C2/[C@@H](c1ccc(N(C)C)cc1)C[C@@]4([C@@](OC(=O)C)(C(=O)COC)CC[C@H]4[C@@H]2CC3)C)CC5
InChI=1S/C31H39NO5/c1-19(33)37-31(28(35)18-36-5)15-14-27-25-12-8-21-16-23(34)11-13-24(21)29(25)26(17-30(27,31)2)20-6-9-22(10-7-20)32(3)4/h6-7,9-10,16,25-27H,8,11-15,17-18H2,1-5H3/t25-,26+,27-,30-,31-/m0/s1
Y Key:JVBGZFRPTRKSBB-MJBQOYBXSA-N
Y
Telapristone (INN ), as telapristone acetate (proposed brand names Proellex , Progenta ; former code name CDB-4124 ), is a synthetic , steroidal selective progesterone receptor modulator (SPRM) related to mifepristone which is under development by Repros Therapeutics for the treatment of breast cancer , endometriosis , and uterine fibroids .[1] [2] It was originally developed by the National Institutes of Health (NIH), and, as of 2017, is in phase II clinical trials for the aforementioned indications.[1] In addition to its activity as an SPRM, the drug also has some antiglucocorticoid activity.[3]
See also [ ]
List of investigational sex-hormonal agents § Progestogenics
Aglepristone
Lilopristone
Onapristone
Toripristone
References [ ]
External links [ ]
Progestogens and antiprogestogens
Progestogens (and progestins )
PR agonists
Retroprogesterone derivatives: Dydrogesterone
Trengestone
Testosterone derivatives: Estranes: Danazol
Dimethisterone
Ethisterone
19-Nortestosterone derivatives: Estranes: Allylestrenol
Altrenogest
Dienogest
Etynodiol diacetate
Lynestrenol
Norethisterone (norethindrone) #
Norethisterone acetate
Norethisterone enanthate
Noretynodrel
Norgesterone
Norgestrienone
Normethandrone (methylestrenolone)
Norvinisterone
Oxendolone
Quingestanol acetate
Tibolone ; Gonanes: Desogestrel
Etonogestrel
Gestodene
Gestrinone
Levonorgestrel #
Norelgestromin
Norgestimate
Norgestrel
Spirolactone derivatives: Drospirenone
Antiprogestogens
SPRMs PR antagonists
Aglepristone
Mifepristone
# WHO-EM
‡ Withdrawn from market
Clinical trials :
† Phase III
§ Never to phase III
See also
Progesterone receptor modulators
Androgens and antiandrogens
Estrogens and antiestrogens
List of progestogens
PR
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
Spirolactone derivatives: Canrenoic acid
Canrenone
Drospirenone
Mespirenone
Potassium canrenoate
Prorenone
SC-5233 (spirolactone)
SC-8109
Spironolactone
Spirorenone
Mixed (SPRMs )
Nonsteroidal: Apigenin
Kaempferol
Naringenin
Syringic acid
Antagonists
Nonsteroidal: Darolutamide
Valproic acid
mPR (PAQR )
See also
Receptor/signaling modulators
Progestogens and antiprogestogens
Androgen receptor modulators
Estrogen receptor modulators
List of progestogens
GR
Agonists Mixed (SEGRMs )
Dagrocorat
Fosdagrocorat
Mapracorat
Antagonists Others
See also
Receptor/signaling modulators
Glucocorticoids and antiglucocorticoids
Mineralocorticoid receptor modulators
List of corticosteroids