Cyproterone acetate 是高活性雄激素受体(AR)拮抗剂,IC50为7.1 nM,还是弱的孕酮受体激动剂。
Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.
0-10 μM
0.2 mg /kg/day皮下注射
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Sonneveld E, et al. Toxicol Sci. 2005, 83(1), 136-148.
[2] Kasper, P., Mueller, L. Carcinogenesis. 20:2185-8 (1999).
分子式 C23H27ClO4 |
分子量 402.91 |
CAS号 427-51-0 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO ≥83 mg/mL |
Water <1 mg/mL |
Ethanol ≥10 mg/mL |
体内溶解度
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NCT02494297 | Hirsutism|Seborrheic Alopecia|Severe Acne|Seborrhea | Center for Epidemiology and Health Research, Germany|Bayer | 2015-03-01 | 2016-11-02 | ||
NCT00919022 | Prostate Cancer | Drug: Cyproterone Acetate (Androcur, BAY94-8367) | Bayer | 2009-08-01 | 2012-10-30 | |
NCT02349399 | Acne Vulgaris | Drug: Cyproterone / Ethinylestradiol (Diane-35, BAY86-5264) and its Generics | Bayer | 2015-05-01 | 2016-03-08 | |
NCT00005623 | Hot Flashes|Prostate Cancer | Drug: cyproterone acetate|Procedure: quality-of-life assessment | Barr Laboratories|National Cancer Institute (NCI) | Phase 3 | 1999-12-01 | 2013-03-25 |
NCT00908674 | Prostate Cancer | Drug: Cyproterone acetate (Androcur) | Bayer | 2008-06-01 | 2010-04-12 | |
NCT01752270 | Polycystic Ovary Syndrome | Drug: Diane-35 pretreatment|Drug: Diane-35 pretreatment | First Affiliated Hospital, Sun Yat-Sen University | Phase 4 | 2012-12-01 | 2012-12-16 |
NCT01573377 | Polycystic Ovary Syndrome|Insulin Resistance | Drug: Metformin|Drug: Ethinylestradiol and Cyproterone Acetate | Chongqing Medical University | 2012-02-01 | 2013-12-26 | |
NCT00752635 | Acne Vulgaris | Drug: Norgestimate-ethinyl estradiol; Cyproterone acetate-ethinyl estradiol | Johnson & Johnson Taiwan Ltd | Phase 4 | 2004-09-01 | 2011-05-18 |
NCT02689843 | Polycystic Ovary Syndrome | Drug: Cyproterone compound + Spironolactone|Drug: Metformin|Drug: Pioglitazone | Shiraz University of Medical Sciences | Early Phase 1 | 2016-03-01 | 2016-08-02 |
NCT00849082 | Prostate Cancer | Drug: cyproterone acetate|Drug: goserelin acetate|Radiation: radiation therapy | European Organisation for Research and Treatment of Cancer - EORTC | Phase 3 | 1987-05-01 | 2012-07-10 |
NCT00363285 | Prostate Cancer | Biological: gonadotrophin releasing hormone|Drug: cyproterone acetate|Procedure: quality-of-life assessment | St. Bartholomew's Hospital|National Cancer Institute (NCI) | Phase 3 | 2003-01-01 | 2013-08-23 |
NCT01011751 | Adenocarcinoma, Prostate | Drug: Cyproterone acetate|Drug: Medroxyprogesterone acetate|Drug: Venlafaxine|Drug: Leuprorelin|Drug: Flutamide|Drug: Placebo | Takeda | Phase 3 | 2004-04-01 | 2015-07-29 |
NCT00955058 | Polycystic Ovary Syndrome | Drug: OCP | Shahid Beheshti University | Phase 2|Phase 3 | 2007-02-01 | 2009-09-01 |
NCT03043924 | Polycystic Ovary Syndrome | Drug: Cyproterone Acetate + estradiol|Drug: Levonorgestrel, Ethinyl Estradiol 0.1-0.02Mg Oral Tablet | University Hospital, Lille|National Research Agency, France | 2017-03-01 | 2017-02-02 | |
NCT02866786 | Polycystic Ovary Syndrome | Drug: Metformin|Drug: ethinyl estradiol and cyproterone acetate | S.C.B. Medical College and Hospital | Phase 4 | 2016-08-01 | 2016-08-31 |
NCT02729545 | Polycystic Ovarian Syndrome | Other: acupuncture|Drug: Diane-35 | Beijing Hospital of Integrated Traditional Chinese and Western Medicine | Phase 2 | 2016-01-01 | 2016-03-31 |
NCT02744131 | Polycystic Ovary Syndrome | Drug: Oral contraceptive pill combination of ethyl estradiol and Cyproterone acetate|Drug: Metformin 1500mgs per day | Kar Clinic & Hospital Pvt. Ltd.|All India Institute of Medical Sciences, New Delhi|Nova IVI Fertility, New Delhi|Dr Patil's Fertility & Endoscopy Clinic, Bangalore|Shreyas Hospital & Sushrut Assisted Conception Clinic, Kolhapur | 2016-05-01 | 2016-08-30 | |
NCT01973816 | Endometriosis | Drug: Triptoreline 11.25 i.v.; Estradiol 0.5% percutaneous gel;|Procedure: rectal shaving; rectal disc excision; colorectal resection|Drug: Cyproterone acetate 50 mg; estradiol 0.5% percutaneous|Drug: Estradiol 0.5% percutaneous gel; Cyproterone acetate 50 mg oral | University Hospital, Rouen | Phase 3 | 2014-11-01 | 2016-08-16 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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