Leflunomide是抗风湿化合物,是嘧啶合成抑制剂。
Leflunomide is a pyrimidine synthesis inhibitor belonging to the DMARD, used as an immunosuppressant agent.
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] Davis JP, et al. Biochemistry, 1996, 35(4), 1270-1273.
[2] Brazelton and Morris (1996) Molecular mechanisms of action of new xenobiotic immunosuppressive drugs: tacrolimus (FK506), sirolimus (rapamycin), mycophenolate mofetil and leflunomide. Curr.Opin.Immunol. 8 710.
[3] Greene et al (1995) Inhibition of dihydroorotate dehydrogenase by the immunosuppressive agent leflunomide. Biochem.Pharmacol. 50 861.
分子式 C12H9F3N2O2 |
分子量 270.21 |
CAS号 75706-12-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 54 mg/mL |
Water <1 mg/mL |
Ethanol 54 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02024334 | Juvenile Idiopathic Arthritis | Drug: Leflunomide | Mashhad University of Medical Sciences | Phase 4 | 2013-06-01 | 2013-12-25 |
NCT00563849 | Rheumatoid Arthritis | Drug: Leflunomide | Sanofi | Phase 4 | 2003-05-01 | 2007-12-03 |
NCT02703194 | Immunoglobulin G4 Related Sclerosing Disease | Drug: Prednisone|Drug: Leflunomide | Chinese PLA General Hospital | Phase 4 | 2016-03-01 | 2016-03-30 |
NCT02509052 | Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma | Other: Laboratory Biomarker Analysis|Drug: Leflunomide|Other: Pharmacological Study | City of Hope Medical Center|National Cancer Institute (NCI) | Phase 1|Phase 2 | 2015-11-01 | 2016-12-23 |
NCT00637819 | Systemic Lupus Eythematosus (SLE) | Drug: Leflunomide | Sanofi | Phase 2 | 2003-01-01 | 2008-03-27 |
NCT01611675 | Melanoma | Drug: Vemurafenib|Drug: Leflunomide | Massachusetts General Hospital | Phase 1|Phase 2 | 2012-07-01 | 2016-09-13 |
NCT01172002 | Nephritis|Lupus | Drug: Leflunomide|Drug: Azathioprine | RenJi Hospital|Changhai Hospital|Shanghai 10th People's Hospital|Shanghai Zhongshan Hospital|The First Affiliated Hospital with Nanjing Medical University|The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School|The First Affiliated Hospital of Soochow University|Zhejiang University|Second Affiliated Hospital, School of Medicine, Zhejiang University|First Affiliated Hospital of Wenzhou Medical Univeristy|Qilu Hospital|AnHui ShengLi Hospital|First Affiliated Hospital Bengbu Medical College|The First Affiliated Hospital of Anhui Medical University | 2010-03-01 | 2010-08-10 | |
NCT00579878 | Rheumatoid Arthritis | Drug: Leflunomide|Drug: Methotrexate-Sulfasalazine-Hydroxychloroquine|Drug: Leflunomide-Sulfasalazine-Hydroxychloroquine|Drug: Leflunomide | University of Nebraska | Phase 3 | 1999-12-01 | 2014-01-02 |
NCT00653003 | To Determine Bioequivalence Under Fed Conditions. | Drug: Leflunomide|Drug: ARAVA | Par Pharmaceutical, Inc.|Novum Pharmaceutical Research Services | Phase 1 | 2003-12-01 | 2008-04-03 |
NCT00834418 | Healthy | Drug: Leflunomide 20 mg Tablets|Drug: ARAVA鈩?20 mg Tablets | Teva Pharmaceuticals USA | Phase 1 | 2002-06-01 | 2009-09-09 |
NCT01659242 | Rheumatoid Arthritis | Drug: Methotrexate plus sulfasalazine|Drug: Leflunomide | Singapore General Hospital | Phase 4 | 2012-07-01 | 2014-11-26 |
NCT00280644 | Arthritis, Rheumatoid | Drug: Leflunomide | Sanofi | Phase 4 | 2004-04-01 | 2011-01-10 |
NCT00802243 | Bullous Pemphigoid | Drug: leflunomide | University Hospital, Limoges | Phase 2 | 2007-09-01 | 2008-12-03 |
NCT00596206 | Arthritis, Rheumatoid | Drug: leflunomide | Sanofi | Phase 3 | 2007-12-01 | 2010-10-11 |
NCT00001863 | Uveitis | Drug: Leflunomide | National Eye Institute (NEI)|National Institutes of Health Clinical Center (CC) | Phase 2 | 1999-03-01 | 2008-03-03 |
NCT00652665 | To Determine the Bioequivalence Study Under Fasting | Drug: Leflunomide|Drug: ARAVA | Par Pharmaceutical, Inc.|Novum Pharmaceutical Research Services | Phase 1 | 2003-06-01 | 2008-04-03 |
NCT01342016 | Lupus Nephritis | Drug: tacrolimus capsule|Drug: tacrolimus placebo|Drug: leflunomide tablet|Drug: leflunomide placebo|Drug: prednisone | Astellas Pharma Inc|Astellas Pharma China, Inc. | Phase 3 | 2011-04-01 | 2014-10-15 |
NCT00946686 | Rheumatoid Arthritis|Psoriatic Arthritis | Drug: Leflunomide 20 mg Tablets (Geneva Pharmaceutical)|Drug: Arava 20 mg Tablets (Aventis Pharmaceutical, Inc.) | Sandoz | Phase 1 | 2002-09-01 | 2009-07-24 |
NCT01727193 | Myasthenia Gravis | Drug: Azathioprine|Drug: Leflunomide | First Affiliated Hospital, Sun Yat-Sen University | Phase 3 | 2012-09-01 | 2012-11-16 |
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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