cyproviron
Clinical trial activity
31 trials · 58 clinical orgs · 0 marketing orgs
Earliest trial started May 1, 1987 (NCT00849082)
Timeline
Indications
Approved for
Studied for
- Acne Vulgaris · Phase 3
- Amenorrhea · Phase 4
- Dysmenorrhea · Phase 4
- Endometrial Hyperplasia · Phase 2/Phase 3
- Endometrial Neoplasms · Phase 2/Phase 3
- Endometriosis · Phase 3
- Gender Dysphoria · Phase 4
- Hot Flashes · Phase 3
- Hyperandrogenism · Phase 4
- Menstruation Disturbances · Phase 4
- Osteoarthritis, Knee · Phase 4
- Pedophilia · Phase 3
- Perimenopause · Phase 2/Phase 3
- Polycystic Ovary Syndrome · Phase 4
- Progesterone · Phase 2/Phase 3
- Prostatic Neoplasms · Phase 3
- Transsexualism · Phase 4
Mechanism of action
- Progesterone receptorAGONIST
PGR agonist
Cyproterone acetate has been shown to compete with dihydrotestosterone for binding to the androgen receptor and to exhibit progestogenic activities. Cyproterone also suppresses the secretion of gonadotropins and thus interferes with testosterone production. Cyproterone acetate is a potent glucocorticoid receptor antagonist.
Cyproterone acetate is known to possess the following pharmacological activity: Androgen receptor antagonist/very weak partial agonist (IC50 = 57 nM) Progesterone receptor agonist (Kd = 15 nM; IC50 = 79 nM) Glucocorticoid receptor antagonist (Kd = 45 nM; IC50 = 360 nM) Weak inhibitor of 3ß-hydroxysteroid dehydrogenase, 17¿-hydroxylase/17,20-lyase, and 21-hydroxylase
- Androgen ReceptorANTAGONIST
AR antagonist
Cyproterone acetate has been shown to compete with dihydrotestosterone for binding to the androgen receptor and to exhibit progestogenic activities. Cyproterone also suppresses the secretion of gonadotropins and thus interferes with testosterone production. Cyproterone acetate is a potent glucocorticoid receptor antagonist.
Cyproterone acetate is known to possess the following pharmacological activity: Androgen receptor antagonist/very weak partial agonist (IC50 = 57 nM) Progesterone receptor agonist (Kd = 15 nM; IC50 = 79 nM) Glucocorticoid receptor antagonist (Kd = 45 nM; IC50 = 360 nM) Weak inhibitor of 3ß-hydroxysteroid dehydrogenase, 17¿-hydroxylase/17,20-lyase, and 21-hydroxylase
- Glucocorticoid receptorANTAGONIST
NR3C1 antagonist
Cyproterone acetate has been shown to compete with dihydrotestosterone for binding to the androgen receptor and to exhibit progestogenic activities. Cyproterone also suppresses the secretion of gonadotropins and thus interferes with testosterone production. Cyproterone acetate is a potent glucocorticoid receptor antagonist.
Cyproterone acetate is known to possess the following pharmacological activity: Androgen receptor antagonist/very weak partial agonist (IC50 = 57 nM) Progesterone receptor agonist (Kd = 15 nM; IC50 = 79 nM) Glucocorticoid receptor antagonist (Kd = 45 nM; IC50 = 360 nM) Weak inhibitor of 3ß-hydroxysteroid dehydrogenase, 17¿-hydroxylase/17,20-lyase, and 21-hydroxylase
Chemistry & pharmacology
SMILES
CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C=C(Cl)C4=CC(=O)[C@@H]5C[C@@H]5[C@]4(C)[C@H]3CC[C@@]21C- Mol. weight
- 416.95 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL142130 ↗
- ChEMBLCHEMBL139835 ↗
Also known as
- androcur
- androcur
- androcur 10
- cyprostat
- cyprostat
- cyproterone
- cyproterone
- cyproterone
- cyproterone 17-o-acetate
- cyproterone 17-o-acetate
- cyproterone acetate
- cyproterone acetate
- cyproterone acetate
- cyproterone acetate
- cyproterone acetate
- cyproterone acetate
- cyproterone acetate
- cyproterone acetate
- cyproterone acetate - ethinyl estradiol
- cyproterone acetate, ethinyl estradiol drug combination
- cyproviron
- diane
- diane
- diane
- diane-35
- diane-35 diario
- sh-714
- sh-714
- shb 209 ae
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05316935 | Phase 2/Phase 3 (Phase 3) | Jul 13, 2022 | Fudan University |
| NCT04831151 | N/A | Mar 1, 2021 | Inonu University |
| NCT03043924 | N/A | Sep 1, 2017 | National Research Agency, France, University of Lille |
| NCT02715232 | Phase 4 | Feb 6, 2017 | University of Vienna |
| NCT03264638 | Phase 2 | Oct 1, 2016 | Chinese Academy of Medical Sciences, People's Liberation Army of China, Sun Yat-Sen University |
| NCT02866786 | Phase 4 | Aug 15, 2016 | SCB Medical College, Cuttack |
| NCT02744131 | N/A | May 1, 2016 | All India Institute of Medical Sciences, Dr Patil's Fertility & Endoscopy Clinic, Bangalore, Kar Clinic & Hospital Pvt. Ltd., Nova IVI Fertility LLC, Shreyas Hospital & Sushrut Assisted Conception Clinic, Kolhapur |
| NCT02689843 | Early Phase 1 (Phase 1) | Mar 1, 2016 | University of Tehran |
| NCT02729545 | Phase 2 | Jan 1, 2016 | Capital Medical University |
| NCT02460445 | N/A | Jan 1, 2015 | Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal, Universidad Carlos III Madrid, Universidad Complutense de Madrid |
| NCT01973816 | Phase 3 | Nov 1, 2014 | Rouen Normandy University |
| NCT02049606 | Phase 4 | Feb 1, 2014 | Catholic University of Korea, Chung-Ang University, Inje University, PMG Pharm Co., Ltd, Seoul National University, University of Ulsan |
| NCT02027337 | Phase 4 | Dec 1, 2013 | Tyumen State Medical Academy |
| NCT01933204 | Phase 2/Phase 3 (Phase 3) | Sep 1, 2013 | Chengdu University of Traditional Chinese Medicines, People's Liberation Army of China, Sichuan University |
| NCT01752270 | Phase 4 | Dec 1, 2012 | Sun Yat-Sen University |
| NCT01768468 | Phase 4 | Oct 1, 2012 | Ajou University, Hanyang University, Keimyung University, Korea University, PMG Pharm Co., Ltd, Seoul National University, Sungkyunkwan University |
| NCT01573377 | N/A | Feb 1, 2012 | Chongqing Medical University |
| NCT01065220 | Phase 4 | Feb 1, 2010 | University of Vienna |
| NCT01103518 | Phase 4 | Dec 1, 2009 | Fundação Educacional Serra dos Órgãos |
| NCT00601276 | Phase 3 | Dec 1, 2007 | Government of France, Institut National de la Santé Et de la Recherche Médicale, France, University of Paris |