Exemestane是芳香酶(aromatase)抑制剂,能抑制人胎盘和鼠卵巢芳香酶,IC50分别为30 nM和40 nM。
Exemestane is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
1 μM
100 mg/kg肌肉注射
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] Di Salle E, et al. J Steroid Biochem Mol Biol, 1994, 49(4-6), 289-294.
分子式 C20H24O2 |
分子量 296.4 |
CAS号 107868-30-4 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 55 mg/mL |
Water <1 mg/mL |
Ethanol 15 mg/mL |
体内溶解度
NCT00810706 | Breast Cancer | Drug: exemestane | Hellenic Breast Surgeons Society | Phase 3 | 2001-04-01 | 2008-12-16 |
NCT01655004 | Breast Carcinoma | Drug: Exemestane | National University Hospital, Singapore | 2012-08-01 | 2016-06-21 | |
NCT01965080 | Endometrial Cancer | Drug: Exemestane | Nordic Society for Gynaecologic Oncology | Phase 2 | 2004-03-01 | 2013-10-15 |
NCT01760980 | Healthy | Drug: Reference product (A) Aromasin (Exemestane)|Drug: Test product (B) Exemestane | Actavis Inc. | Phase 1 | 2012-11-01 | 2014-05-27 |
NCT00201773 | Breast Cancer | Drug: Exemestane|Drug: Celecoxib|Other: Correlative studies | Ohio State University Comprehensive Cancer Center|Pfizer | Phase 2 | 2003-07-01 | 2015-06-25 |
NCT01648608 | Breast Cancer | Drug: Exemestane | Tianjin Medical University | Phase 2|Phase 3 | 2012-01-01 | 2012-08-02 |
NCT01743560 | Oestrogen Receptor Positive Advanced Breast Cancer | Drug: RAD001|Drug: Exemestane | Novartis Pharmaceuticals|Novartis | Phase 4 | 2013-01-01 | 2016-02-24 |
NCT00676663 | Breast Cancer|Estrogen Receptor-Positive Breast Cancer|Breast Cancer, Estrogen Receptor-Positive|ER+ Breast Cancer | Drug: entinostat|Drug: exemestane | Syndax Pharmaceuticals | Phase 2 | 2008-05-01 | 2014-03-19 |
NCT00073073 | Breast Neoplasms | Drug: Exemestane|Dietary Supplement: Calcium carbonate|Dietary Supplement: Vitamin D | Georgetown University|National Cancer Institute (NCI) | Phase 2 | 2003-11-01 | 2016-04-11 |
NCT00200174 | Breast Cancer | Drug: Raloxifene followed by combination therapy|Drug: Exemestane followed by combination therapy | Memorial Sloan Kettering Cancer Center|Pharmacia | 1999-07-01 | 2015-12-21 | |
NCT00919399 | Breast Neoplasms | Drug: Exemestane|Drug: tamoxifen | Institut Claudius Regaud|PHARMACIA SAS | Phase 2 | 2002-01-01 | 2009-06-11 |
NCT01431053 | Breast Neoplasms | Drug: aspirin|Drug: Exemestane | Chinese Academy of Medical Sciences | Phase 2 | 2011-07-01 | 2013-03-12 |
NCT00201864 | Breast Cancer | Drug: Exemestane|Drug: Fulvestrant | Ewa Mrozek|Pfizer|Ohio State University Comprehensive Cancer Center | Phase 2 | 2005-09-01 | 2016-07-14 |
NCT02990845 | Premenopausal Breast Cancer | Drug: Pembrolizumab/ Exemestane/ Leuprolide | National Taiwan University Hospital|Merck Sharp & Dohme Corp. | Phase 1|Phase 2 | 2016-12-01 | 2016-12-08 |
NCT01658176 | Breast Neoplasms | Drug: PF-04691502|Drug: Exemestane|Drug: Exemestane | Pfizer | Phase 2 | 2013-01-01 | 2012-10-26 |
NCT02025712 | Hormone Receptor Positive Malignant Neoplasm of Breast | Drug: Exemestane|Drug: Everolimus | Organisation for Oncology and Translational Research | Phase 2 | null | 2013-12-29 |
NCT01155063 | Early Breast Cancer | Other: Aromasin (exemestane) | Pfizer | 2010-09-01 | 2012-09-25 | |
NCT00031889 | Prostate Cancer | Drug: Exemestane|Drug: Exemestane+bicalutamide | Swiss Group for Clinical Cancer Research | Phase 2 | 2001-08-01 | 2012-05-14 |
NCT00767520 | Breast Cancer | Drug: Exemestane + Dasatinib|Drug: Exemestane + Placebo | Bristol-Myers Squibb | Phase 2 | 2009-02-01 | 2013-02-22 |
NCT00649090 | Breast Neoplasms | Drug: exemestane | Pfizer | Phase 4 | 2005-03-01 | 2008-09-25 |
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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