Bardoxolone Methyl是一种IKK抑制剂,具有强效的促凋亡和抗炎活性。
Bardoxolone Methyl is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities. Phase 3.
~5 μM
~60 mg/kg 口服给药
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] Honda T, et al. J Med Chem. 2000, 43(22), 4233-4246.
[2] Prevention of prostate cancer with oleanane synthetic triterpenoid CDDO-Me in the TRAMP mouse model of prostate cancer By Gao, Xiaohua; Deeb, Dorrah; Liu, Yongbo; Arbab, Ali S.; Divine, George W.; Dulchavsky, Scott A.; Gautam, Subhash C.From Cancers (Basel). 2011; 3(3): 3353-3369
分子式 C32H43NO4 |
分子量 505.69 |
CAS号 218600-53-4 |
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 |
NCT03068130 | Pulmonary Hypertension | Drug: Bardoxolone methyl | Reata Pharmaceuticals, Inc. | Phase 3 | 2017-04-01 | 2017-03-06 |
NCT00529438 | Advanced Solid Tumors|Lymphoid Malignancies | Drug: Bardoxolone methyl | Reata Pharmaceuticals, Inc. | Phase 1 | 2006-04-01 | 2014-11-04 |
NCT03019185 | Alport Syndrome | Drug: Placebo Oral Capsule|Drug: Bardoxolone Methyl | Reata Pharmaceuticals, Inc. | Phase 2|Phase 3 | 2017-03-02 | 2017-03-15 |
NCT02657356 | Connective Tissue Disease-Associated Pulmonary Arterial Hypertension | Drug: Placebo capsules|Drug: Bardoxolone methyl capsules | Reata Pharmaceuticals, Inc. | Phase 3 | 2016-09-01 | 2017-03-09 |
NCT01461161 | Healthy Volunteers | Drug: bardoxolone methyl | Reata Pharmaceuticals, Inc. | Phase 1 | 2011-10-01 | 2012-03-30 |
NCT01053936 | Renal Insufficiency, Chronic|Diabetes Mellitus, Type 2 | Drug: Bardoxolone methyl (amorphous dispersion) | Reata Pharmaceuticals, Inc. | Phase 2 | 2010-01-01 | 2012-06-12 |
NCT00811889 | Chronic Kidney Disease|Type 2 Diabetes|Diabetic Nephropathy | Other: Placebo|Drug: Bardoxolone Methyl (RTA 402) | Reata Pharmaceuticals, Inc. | Phase 2 | 2009-04-01 | 2012-06-12 |
NCT02036970 | Pulmonary Arterial Hypertension|Pulmonary Hypertension | Drug: Bardoxolone methyl|Drug: Placebo | Reata Pharmaceuticals, Inc. | Phase 2 | 2014-05-01 | 2017-03-08 |
NCT00664027 | Diabetic Nephropathy | Drug: RTA 402 (Bardoxolone Methyl) | Reata Pharmaceuticals, Inc. | Phase 2 | 2008-04-01 | 2012-11-29 |
NCT01351675 | Renal Insufficiency, Chronic|Diabetes Mellitus, Type 2 | Drug: Placebo|Drug: Bardoxolone Methyl: 20 mg | Reata Pharmaceuticals, Inc. | Phase 3 | 2011-06-01 | 2014-04-28 |
NCT01549769 | Renal Insufficiency, Chronic|Diabetes Mellitus, Type 2 | Drug: Bardoxolone Methyl | Reata Pharmaceuticals, Inc. | Phase 1 | 2012-04-01 | 2014-04-28 |
NCT01563562 | Hepatic Impairment|Healthy | Drug: Bardoxolone Methyl | Reata Pharmaceuticals, Inc. | Phase 1 | 2012-04-01 | 2013-04-09 |
NCT02316821 | Chronic Kidney Disease|Type 2 Diabetes | Drug: RTA 402|Drug: Placebo | Kyowa Hakko Kirin Co., Ltd | Phase 2 | 2014-12-01 | 2017-01-03 |
NCT00535314 | Malignant Melanoma | Drug: RTA 402 Dose1|Drug: RTA 402 Dose2 | Reata Pharmaceuticals, Inc. | Phase 2 | null | 2014-10-27 |
NCT00508807 | Lymphoid Malignancies|Solid Tumors | Drug: RTA 402 | M.D. Anderson Cancer Center|Reata Pharmaceuticals, Inc. | Phase 1 | 2006-04-01 | 2012-07-27 |
NCT01551446 | Renal Insufficiency, Chronic|Diabetes Mellitus, Type 2 | Drug: Bardoxolone Methyl | Reata Pharmaceuticals, Inc. | Phase 1 | 2012-04-01 | 2012-11-01 |
NCT00550849 | Liver Disease | Drug: RTA 402|Drug: RTA 402|Drug: RTA 402 | Reata Pharmaceuticals, Inc. | Phase 1|Phase 2 | 2007-04-01 | 2007-11-06 |
NCT01503866 | Healthy | Drug: bardoxolone methyl | Reata Pharmaceuticals, Inc. | Phase 1 | 2011-12-01 | 2011-12-31 |
NCT01572610 | Chronic Kidney Disease|Type 2 Diabetes | Drug: RTA 402 | Kyowa Hakko Kirin Co., Ltd | Phase 2 | 2012-02-01 | 2017-02-28 |
NCT01574365 | Chronic Kidney Disease|Type 2 Diabetes | Drug: RTA 402 | Kyowa Hakko Kirin Co., Ltd | Phase 2 | 2012-02-01 | 2017-02-28 |
NCT00529113 | Pancreatic Neoplasms|Pancreatic Cancer | Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Gemcitabine|Drug: Placebo|Drug: Bardoxolone methyl | Reata Pharmaceuticals, Inc. | Phase 1|Phase 2 | 2007-09-01 | 2014-11-13 |
NCT01655186 | Renal Insufficiency, Chronic|Diabetes Mellitus, Type 2 | Drug: Bardoxolone Methyl|Drug: Placebo | Reata Pharmaceuticals, Inc. | Phase 2 | 2012-09-01 | 2012-10-19 |
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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