Ketoconazole (酮康唑)是咪唑类抗真菌剂,是经典的CYP3A4抑制剂。
Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.
25 μM
25 mg/kg 腹腔注射
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] Ayub and Levell (1989) Inhibition of human adrenal steroidogenic enzymes in vitro by imidazole drugs including ketoconazole. J.Steroid Biochem. 32 515.
[2] Kuhn-Velten et al (1992) Ketoconazole inhibition of the bifunctional cytochrome P450c17 does not affect androgen formation from the endogenous lyase substrate. Biochem.Pharmacol. 44 2371.
[3] Dumaine et al (1998) Blockade of HERG and Kv1.5 by ketoconazole. J.Pharmacol.Exp.Ther. 286 727.
分子式 C26H28Cl2N4O4 |
分子量 531.43 |
CAS号 65277-42-1 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 20 mg/mL |
Water <1 mg/mL |
Ethanol 20 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00830388 | Tinea Versicolor | Drug: Ketoconazole 2% Foam | Boni Elewski, MD|University of Alabama at Birmingham | Phase 4 | 2008-11-01 | 2012-08-21 |
NCT01330563 | Type 2 Diabetes Mellitus | Drug: CKD-501, Ketoconazole | Chong Kun Dang Pharmaceutical|Severance Hospital | Phase 1 | 2011-03-01 | 2011-06-28 |
NCT00895310 | Prostate Cancer | Drug: Ketoconazole | University of California, Davis | Phase 2 | 2009-05-01 | 2016-12-22 |
NCT01735240 | Asthma,|Pharmacokinetics,|Cmax,|Tmax,|位z,|AUC,|Ketoconazole,|Metabolite | Drug: AZD5069|Drug: Ketoconazole | AstraZeneca | Phase 1 | 2012-12-01 | 2015-06-24 |
NCT01584297 | Granulosa Cell Tumour of the Ovary | Drug: Ketoconazole | Grupo Espaol de Tumores Hurfanos e Infrecuentes | Phase 2 | 2012-10-01 | 2015-01-19 |
NCT01036594 | Prostate Cancer | Drug: Ketoconazole, hydrocortisone|Drug: Ketoconazole, dexamethasone | University of California, San Francisco | Phase 2 | 2009-12-01 | 2016-05-22 |
NCT01910480 | Effect of Ketoconazole on the PK of NBI-98854 in Healthy Subjects | Drug: NBI-98854 50 mg capsule once daily|Drug: Ketoconazole 400 mg (200 mg twice daily) | Neurocrine Biosciences | Phase 1 | 2013-07-01 | 2013-09-03 |
NCT01154764 | Healthy | Drug: CG100649|Drug: CG100649 and ketoconazole | CrystalGenomics, Inc. | Phase 1 | 2009-10-01 | 2013-02-13 |
NCT00212095 | Metastatic Breast Cancer | Drug: docetaxel and ketoconazole | National University Hospital, Singapore | Phase 2 | 2005-06-01 | 2012-10-31 |
NCT00824863 | Pityrosporum Folliculitis | Drug: ketoconazole 2% foam | Wayne Fujita, M.D.|Fujita, Wayne, M.D. | Phase 4 | 2008-12-01 | 2014-08-19 |
NCT01318265 | Pharmacokinetics | Drug: Regorafenib (BAY73-4506); Regorafenib (BAY73-4506) plus ketoconazole | Bayer | Phase 1 | 2011-03-01 | 2014-10-31 |
NCT01657838 | Pharmacokinetics of Isavuconazole|Pharmacokinetics of Ketoconazole|Healthy Adult Volunteers | Drug: Isavuconazole|Drug: Ketoconazole | Astellas Pharma Global Development, Inc.|Basilea Pharmaceutica International Ltd|Astellas Pharma Inc | Phase 1 | 2012-05-01 | 2015-08-31 |
NCT00388557 | Cancer | Drug: vinflunine + ketaconazole | Bristol-Myers Squibb | Phase 1 | 2005-10-01 | 2016-09-16 |
NCT00404378 | Nausea and Vomiting, Chemotherapy-Induced | Drug: ketoconazole|Drug: casopitant | GlaxoSmithKline | Phase 1 | 2006-10-01 | 2016-10-26 |
NCT00703846 | Dermatitis, Seborrheic | Drug: Ketoconazole | Stiefel, a GSK Company|GlaxoSmithKline | Phase 4 | 2008-06-01 | 2016-12-01 |
NCT01468558 | Healthy | Drug: MAP0004|Drug: IV DHE|Drug: Ketoconazole | Allergan|MAP Pharmaceuticals, Inc., a wholly owned subsidiary of Allergan | Phase 1 | 2010-07-01 | 2013-12-09 |
NCT01896323 | Healthy Volunteers | Drug: CC-223|Drug: Ketoconazole | Celgene Corporation|Celgene | Phase 1 | 2013-07-01 | 2014-04-03 |
NCT01021358 | Lymphoma|Chronic Lymphocytic Leukemia|Solid Tumors | Drug: ABT-263|Drug: Ketoconazole | Abbott | Phase 1 | 2010-01-01 | 2010-12-16 |
NCT00384917 | Healthy | Drug: Ketoconazole | Wyeth is now a wholly owned subsidiary of Pfizer | Phase 1 | 2006-08-01 | 2009-07-08 |
NCT00501397 | Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2 | Drug: ketoconazole|Drug: GSK189075 | GlaxoSmithKline | Phase 1 | 2007-02-01 | 2012-05-31 |
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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