Apremilast是一种口服生物有效的PDE4和TNF-α抑制剂,IC50分别为74 nM和77 nM。
Apremilast (CC-10004) is a potent and orally active PDE4 and TNF-α inhibitor with IC50 of 74 nM and 77 nM, respectively.
~10 μM
5 mg/kg/day,分成每天两次的剂量口服处理
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] Man HW, et al. J Med Chem, 2009,52(6), 1522-1524.
分子式 C22H24N2O7S |
分子量 460.5 |
CAS号 608141-41-9 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 90 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 |
NCT01634191 | Healthy Volunteer | Drug: Apremilast | Celgene Corporation | Phase 1 | 2012-02-01 | 2016-03-24 |
NCT01634178 | Healthy Volunteer | Drug: Apremilast|Drug: Apremilast | Celgene Corporation|Celgene | Phase 1 | 2012-02-01 | 2012-07-05 |
NCT02576678 | Psoriasis | Drug: Apremilast | Celgene | Phase 2 | 2015-10-01 | 2017-01-30 |
NCT00521339 | Psoriasis-Type Psoriasis|Plaque-Type Psoriasis | Drug: Apremilast | Celgene Corporation | Phase 2 | 2007-08-01 | 2016-10-27 |
NCT01925768 | Psoriatic Arthritis | Drug: Apremilast 30 mg|Drug: Placebo | Celgene Corporation | Phase 3 | 2013-09-01 | 2016-08-10 |
NCT01561963 | Healthy | Drug: Apremilast|Drug: Rifampin | Celgene Corporation | Phase 1 | 2012-02-01 | 2016-11-21 |
NCT00931242 | Atopic Dermatitis|Allergic Contact Dermatitis | Drug: Apremilast | Tufts Medical Center|Celgene Corporation | Phase 2 | 2009-06-01 | 2010-11-23 |
NCT03082729 | Psoriasis|Cardiovascular Diseases | Drug: Apremilast | University of Pennsylvania|Celgene Corporation|National Heart, Lung, and Blood Institute (NHLBI) | Phase 4 | 2017-04-01 | 2017-03-10 |
NCT01200264 | Chronic Plaque Psoriasis | Drug: apremilast | Duke University | Phase 2 | 2010-09-01 | 2014-07-14 |
NCT01250548 | Rheumatoid Arthritis | Biological: apremilast|Other: Placebo | Baylor Research Institute | Phase 2 | 2010-05-01 | 2014-09-02 |
NCT02775500 | Psoriatic Arthritis|Psoriasis | Drug: apremilast | University of California, San Diego|Celgene|The Organization of Teratology Information Specialists | 2014-11-01 | 2017-03-22 | |
NCT01074502 | Acne | Drug: apremilast | University of North Carolina, Chapel Hill|Celgene | Phase 2 | 2010-02-01 | 2017-02-01 |
NCT02236988 | Healthy Volunteers | Drug: Apremilast | Celgene Corporation | Phase 1 | 2014-01-01 | 2016-03-24 |
NCT02400749 | Palmo-plantar Psoriasis | Drug: Apremilast|Drug: Placebo | Innovaderm Research Inc.|Celgene | Phase 4 | 2015-05-01 | 2017-02-06 |
NCT03000309 | Plaque Psoriasis | Drug: Apremilast | Derm Research, PLLC|Celgene | Phase 4 | 2016-12-29 | 2017-03-16 |
NCT02307513 | Behcet Syndrome | Drug: Apremilast (CC-10004)|Drug: Placebo | Celgene Corporation | Phase 3 | 2014-12-01 | 2016-12-28 |
NCT02641353 | Healthy Volunteers | Drug: Apremilast|Drug: Apremilast Oral Suspension | Celgene Corporation | Phase 1 | 2016-01-01 | 2016-03-25 |
NCT01212770 | Psoriatic Arthritis | Drug: Apremilast 20mg|Drug: Apremilast 30mg|Drug: Placebo | Celgene | Phase 3 | 2010-09-01 | 2017-01-17 |
NCT01232283 | Plaque Psoriasis | Drug: Apremilast|Drug: Placebo|Other: Topical or Phototherapy Therapy | Celgene | Phase 3 | 2010-11-01 | 2017-01-09 |
NCT01307423 | Psoriatic Arthritis | Drug: Apremilast 20mg|Drug: Apremilast 30mg|Drug: Placebo | Celgene | Phase 3 | 2010-12-01 | 2017-01-17 |
NCT00606450 | Psoriasis | Drug: CC-10004|Drug: CC-10004|Drug: Placebo | Celgene Corporation|Celgene | Phase 2 | 2006-04-01 | 2013-05-29 |
NCT02425826 | Parapsoriasis | Drug: Apremilast|Drug: Placebo | Celgene Corporation | Phase 4 | 2015-04-01 | 2016-08-09 |
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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