AZ-5104是一种有效的EGFR抑制剂, 在体内外具有抗肿瘤活性。
AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.
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] Cross DA, et al. Cancer Discov. 2014, 4(9), 1046-1061.
[2] Ivana Sullivan,et al. Next-Generation EGFR Tyrosine Kinase Inhibitors for Treating EGFR-Mutant Lung Cancer beyond First Line. Front Med (Lausanne) 2016; 3: 76. Published online 2017 Jan 18. doi: 10.3389/fmed.2016.00076.
分子式 C27H31N7O2 |
分子量 485.58 |
CAS号 1421373-98-9 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 89 mg/mL |
Water <1 mg/mL |
Ethanol 18 mg/mL |
体内溶解度
NCT02529995 | Carcinoma, Non-Small-Cell Lung With EGFR Mutation Positive | Drug: AZD9291 40 mg|Drug: AZD9291 80 mg | AstraZeneca | Phase 1 | 2015-08-01 | 2017-01-13 |
NCT02197247 | Non Small Cell Lung Cancer | Procedure: Pharmacokinetic sampling - AZD9291|Drug: Rifampicin|Drug: AZD9291 tablet dosing|Procedure: Pharmacokinetic sampling - rifampicin|Procedure: Pharmacokinetic sampling - AZ5140 and AZ7550 | AstraZeneca | Phase 1 | 2014-12-01 | 2017-02-03 |
NCT02161770 | Solid Tumours | Drug: AZD9291 tablet dosing|Procedure: Pharmacokinetic sampling - AZD9291|Procedure: Pharmacokinetic sampling - AZ5140 and AZ7550 | AstraZeneca | Phase 1 | 2014-12-22 | 2017-03-21 |
NCT02163733 | Advanced Non Small Cell Lung Cancer|Advanced (Inoperable) Non Small Cell Lung Cancer | Drug: AZD9291 tablets|Procedure: Pharmacokinetic sampling - AZD9291|Other: Dietary Fasted|Other: Dietary High Fat|Procedure: Pharmacokinetic sampling - AZ5140 and AZ7550 | AstraZeneca | Phase 1 | 2014-11-01 | 2017-02-03 |
NCT02491944 | Oncology | Drug: AZD9291|Drug: [14C]AZD9291 | AstraZeneca | Phase 1 | 2015-07-01 | 2016-08-19 |
NCT02224053 | Healthy Volunteer | Procedure: Pharmacokinetic sampling - AZD9291|Drug: AZD9291 tablet dosing|Drug: Omeprazole tablet dosing|Procedure: Pharmacokinetic sampling - AZ5140 and AZ7550 | AstraZeneca | Phase 1 | 2014-09-01 | 2016-05-23 |
NCT02317016 | Non Small Cell Lung Cancer | Procedure: Pharmacokinetic sampling - AZD9291|Drug: AZD9291 tablet dosing|Drug: Rosuvastatin|Procedure: Pharmacokinetic sampling - rosuvastatin|Procedure: Pharmacokinetic sampling - AZ5140 and AZ7550 | AstraZeneca | Phase 1 | 2015-03-01 | 2017-02-03 |
NCT02157883 | Advanced Non Small Cell Lung Cancer|Advanced (Inoperable) Non Small Cell Lung Cancer | Procedure: Pharmacokinetic sampling|Drug: AZD9291|Drug: Itraconazole | AstraZeneca | Phase 1 | 2014-11-01 | 2017-01-09 |
NCT02096679 | Healthy Volunteers | Drug: AZD9291 | AstraZeneca | Phase 1 | 2014-05-01 | 2015-10-01 |
NCT02923947 | Solid Tumours | Drug: Osimertinib; AZD9291 | AstraZeneca|Quintiles, Inc. | Phase 1 | 2017-01-01 | 2016-10-03 |
NCT02908750 | Non Small Cell Lung Cancer | Drug: Fexofenadine tablet dosing|Drug: Osimertininb tablet dosing | AstraZeneca|Quintiles, Inc. | Phase 1 | 2017-01-01 | 2016-09-23 |
NCT02511106 | Stage IB-IIIA Non-small Cell Lung Carcinoma | Drug: AZD9291 80 mg/40 mg|Drug: Placebo AZD9291 80 mg/40 mg | AstraZeneca|Parexel | Phase 3 | 2015-10-01 | 2017-02-28 |
NCT02296125 | Locally Advanced or Metastatic EGFR Sensitising Mutation Positive Non Small Cell Lung Cancer | Drug: AZD9291 80 mg/40 mg + placebo|Drug: Placebo Erlotinib 150/100mg|Drug: Placebo Gefitinib 250 mg|Drug: Erlotinib 150/100 mg|Drug: Gefitinib 250 mg|Drug: Placebo AZD9291 80 mg/ 40 mg | AstraZeneca|Parexel | Phase 3 | 2014-12-03 | 2017-03-20 |
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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