Baricitinib是JAK1和JAK2抑制剂,IC50分别为5.9 nM和5.7 nM,比对JAK3和Tyk2的抑制性高70倍和10倍,对c-Met和Chk2无活性。
Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.
10 mg/mL口服
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] Fridman JS, et al. J Immunol, 2010, 184(9), 5298-5307.
分子式 C16H17N7O2S |
分子量 371.42 |
CAS号 1187594-09-7 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 74 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 |
NCT02340104 | Healthy Volunteers | Drug: Baricitinib|Drug: [^13C4D3^15N]-baricitinib | Eli Lilly and Company | Phase 1 | 2015-01-01 | 2015-03-01 |
NCT01968057 | Healthy Volunteers | Drug: Baricitinib|Drug: Ciclosporin | Eli Lilly and Company | Phase 1 | 2013-10-01 | 2014-01-08 |
NCT01870388 | Liver Diseases|Hepatic Insufficiency | Drug: Baricitinib | Eli Lilly and Company | Phase 1 | 2013-06-01 | 2013-09-10 |
NCT01925144 | Healthy Volunteers | Drug: Baricitinib|Drug: Omeprazole | Eli Lilly and Company | Phase 1 | 2013-10-01 | 2013-11-21 |
NCT02263911 | Healthy Volunteers | Drug: Baricitinib | Eli Lilly and Company | Phase 1 | 2014-11-01 | 2015-01-05 |
NCT03026504 | Arteritis, Giant Cell | Drug: Baricitinib | Matthew J Koster|Eli Lilly and Company|Mayo Clinic | Phase 2 | 2017-02-01 | 2017-01-19 |
NCT01924299 | Healthy Volunteers | Drug: Baricitinib|Drug: Ketoconazole|Drug: Fluconazole | Eli Lilly and Company | Phase 1 | 2013-08-01 | 2013-11-21 |
NCT01859078 | Healthy Volunteers | Drug: Baricitinib|Drug: Digoxin | Eli Lilly and Company | Phase 1 | 2013-05-01 | 2013-08-23 |
NCT01896726 | Healthy Volunteers | Drug: Baricitinib|Drug: Microgynon | Eli Lilly and Company | Phase 1 | 2013-07-01 | 2013-10-18 |
NCT02708095 | Systemic Lupus Erythematosus | Drug: Baricitinib|Drug: Placebo | Eli Lilly and Company | Phase 2 | 2016-03-01 | 2017-03-23 |
NCT01937026 | Healthy Volunteers | Drug: Baricitinib|Drug: Probenecid | Eli Lilly and Company | Phase 1 | 2013-09-01 | 2013-12-03 |
NCT02759731 | Chronic Graft vs Host Disease|Chronic Graft-Versus-Host Disease | Drug: Baricitinib | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) | Phase 1|Phase 2 | 2016-04-08 | 2017-03-08 |
NCT02265705 | Rheumatoid Arthritis | Drug: Baricitinib|Drug: Placebo | Eli Lilly and Company | Phase 3 | 2014-10-01 | 2016-07-01 |
NCT01910311 | Healthy Volunteers | Drug: Baricitinib|Drug: Rifampicin | Eli Lilly and Company | Phase 1 | 2013-08-01 | 2013-10-30 |
NCT01960140 | Healthy Volunteers | Drug: Baricitinib|Drug: Simvastatin | Eli Lilly and Company | Phase 1 | 2013-10-01 | 2014-01-08 |
NCT02576938 | Atopic Dermatitis | Drug: Baricitinib|Drug: Placebo|Drug: Triamcinolone (Optional) | Eli Lilly and Company | Phase 2 | 2016-02-01 | 2017-03-14 |
NCT01885078 | Rheumatoid Arthritis | Drug: Baricitinib|Drug: Placebo | Eli Lilly and Company | Phase 3 | 2013-06-01 | 2017-03-22 |
NCT01683409 | Diabetic Kidney Disease | Drug: baricitinib|Drug: Placebo | Eli Lilly and Company|Incyte Corporation | Phase 2 | 2012-08-01 | 2015-01-16 |
NCT01721044 | Rheumatoid Arthritis | Drug: Placebo|Drug: Baricitinib | Eli Lilly and Company | Phase 3 | 2013-01-01 | 2014-09-29 |
NCT01721057 | Rheumatoid Arthritis | Drug: Placebo|Drug: Baricitinib | Eli Lilly and Company | Phase 3 | 2012-12-01 | 2015-02-19 |
NCT01490632 | Psoriasis|Skin Diseases|Skin Diseases, Papulosquamous | Drug: Placebo|Drug: LY3009104 | Eli Lilly and Company|Incyte Corporation | Phase 2 | 2011-12-01 | 2014-11-25 |
NCT01710358 | Rheumatoid Arthritis | Drug: Placebo|Drug: Adalimumab|Drug: Baricitinib | Eli Lilly and Company | Phase 3 | 2012-10-01 | 2016-05-13 |
NCT01711359 | Rheumatoid Arthritis | Drug: Baricitinib|Drug: Methotrexate|Drug: Placebo|Drug: Folic Acid | Eli Lilly and Company | Phase 3 | 2012-11-01 | 2015-09-24 |
NCT01299285 | Healthy Volunteers | Drug: LY3009104 | Eli Lilly and Company | Phase 1 | 2011-02-01 | 2011-04-06 |
NCT02758613 | Healthy | Drug: LY3009104|Drug: Placebo | Eli Lilly and Company | Phase 1 | 2016-05-01 | 2016-08-25 |
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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