Teriflunomide是Leflunomide的活性代谢物,通过抑制酶二氢乳清酸脱氢酶,从而抑制嘧啶从头合成,作为一种免疫调节剂。
Teriflunomide is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory 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] OJ H, et al. Ther Clin Risk Manag, 2013,9,177-190.
分子式 C12H9F3N2O2 |
分子量 270.21 |
CAS号 108605-62-5 |
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 <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02263547 | Teriflunomide Elimination|Healthy Volunteers | Drug: teriflunomide|Drug: Colestipol | Derrick Scott Robertson|Genzyme, a Sanofi Company|University of South Florida | Phase 1 | 2015-01-01 | 2016-09-15 |
NCT01970410 | Multiple Sclerosis | Drug: teriflunomide | Multiple Sclerosis Center of Northeastern New York|Providence Multiple Sclerosis Center | Phase 4 | 2013-10-01 | 2016-10-24 |
NCT01895335 | Multiple Sclerosis | Drug: Teriflunomide | Sanofi | Phase 4 | 2013-06-01 | 2016-10-10 |
NCT02490982 | Relapsing Remitting Multiple Sclerosis | Drug: Teriflunomide | Centre hospitalier de l'Universit de Montral (CHUM)|Genzyme, a Sanofi Company|Montreal Neurological Institute and Hospital | Phase 4 | 2015-07-01 | 2016-01-25 |
NCT01487096 | Multiple Sclerosis | Drug: Teriflunomide|Drug: Placebo (placebo for teriflunomide) | Sanofi | Phase 2 | 2001-04-01 | 2012-10-03 |
NCT00134563 | Multiple Sclerosis | Drug: Teriflunomide|Drug: Placebo (for teriflunomide) | Sanofi | Phase 3 | 2004-09-01 | 2013-01-02 |
NCT00622700 | Multiple Sclerosis | Drug: Teriflunomide|Drug: Placebo | Sanofi | Phase 3 | 2008-02-01 | 2017-01-20 |
NCT00489489 | Multiple Sclerosis | Drug: Teriflunomide|Drug: Placebo (for Teriflunomide)|Drug: Interferon-尾 | Sanofi | Phase 2 | 2007-05-01 | 2012-11-05 |
NCT00475865 | Multiple Sclerosis | Drug: Teriflunomide|Drug: Placebo (for teriflunomide)|Drug: Glatiramer Acetate (GA) | Sanofi | Phase 2 | 2007-04-01 | 2012-11-05 |
NCT02046629 | Multiple Sclerosis | Drug: Teriflunomide HMR1726|Drug: cholestyramine | Sanofi | Phase 1 | 2014-05-01 | 2014-08-20 |
NCT00751881 | Multiple Sclerosis | Drug: Placebo|Drug: Teriflunomide | Sanofi | Phase 3 | 2008-08-01 | 2016-05-27 |
NCT01252355 | Multiple Sclerosis Relapse | Drug: Teriflunomide|Drug: Placebo (for teriflunomide)|Drug: Interferon-beta (IFN-beta) | Sanofi | Phase 3 | 2011-01-01 | 2014-05-30 |
NCT00803049 | Multiple Sclerosis | Drug: Teriflunomide (HMR1726) | Sanofi | Phase 3 | 2006-10-01 | 2016-12-05 |
NCT02792218 | Relapsing Multiple Sclerosis | Drug: Ofatumumab subcutaneous injection|Drug: Placebo orally matching to teriflunomide|Drug: Teriflunomide orally|Drug: Placebo subcutanous injection matching to ofatumumab | Novartis Pharmaceuticals|Novartis | Phase 3 | 2016-09-19 | 2017-02-22 |
NCT02792231 | Relapsing Multiple Scelrosis | Drug: Ofatumumab subcutaneous injection|Drug: Placebo orally matching to teriflunomide|Drug: Teriflunomide orally|Drug: Placebo subcutaneous injection matching to ofatumumab | Novartis Pharmaceuticals|Novartis | Phase 3 | 2016-08-26 | 2017-02-06 |
NCT00883337 | Multiple Sclerosis | Drug: Interferon -1a|Drug: Teriflunomide | Sanofi | Phase 3 | 2009-04-01 | 2016-05-04 |
NCT01403376 | Multiple Sclerosis | Drug: teriflunomide|Drug: Interferon--1|Biological: Influenza vaccine | Sanofi | Phase 2 | 2011-09-01 | 2016-01-21 |
NCT00228163 | Multiple Sclerosis | Drug: teriflunomide (HMR1726) | Sanofi | Phase 2 | 2002-01-01 | 2015-03-24 |
NCT02201108 | Multiple Sclerosis | Drug: Teriflunomide HMR1726|Drug: Placebo | Genzyme, a Sanofi Company|Sanofi | Phase 3 | 2014-07-01 | 2017-03-09 |
NCT02587195 | Multiple Sclerosis | Drug: Teriflunomide | Centre Hospitalier Universitaire de Nice | Phase 3 | 2015-10-01 | 2015-10-23 |
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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