Neratinib (HKI-272)是一种高度选择性的HER2和EGFR抑制剂,IC50分别为59 nM和92 nM;微弱抑制KDR和Src,对Akt,CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf和c-Met没有显著的抑制作用。
Neratinib (synonym: HKI-272; HKI 272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met.
30% PEG400+0.5% Tween80+5% propylene glycol
0.5 ng/mL-5 μg/mL
~80 mg/kg/day口服饲喂
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] Rabindran SK, et al. Cancer Res, 2004, 64(11), 3958-3965.
分子式 C30H29ClN6O3 |
分子量 557.04 |
CAS号 698387-09-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 5 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 |
NCT01128842 | Advanced Malignant Solid Tumors | Drug: Neratinib + Capecitabine | Puma Biotechnology, Inc. | Phase 1 | 2010-04-01 | 2012-05-10 |
NCT00838539 | Neoplasms|Malignant Carcinoma | Drug: Neratinib|Drug: Temsirolimus | Puma Biotechnology, Inc. | Phase 1 | 2009-04-01 | 2016-11-22 |
NCT02932280 | Solid Tumor|Central Nervous System Tumor|Lymphoma|Leukemia | Drug: Neratinib | Memorial Sloan Kettering Cancer Center|Milton S. Hershey Medical Center|M.D. Anderson Cancer Center|Stanford University|Arkansas Children's Hospital Research Institute|Alberta Children's Hospital|Phoenix Children's Hospital|University of Texas | Phase 1|Phase 2 | 2016-10-01 | 2017-02-15 |
NCT01142063 | Healthy | Drug: Neratinib|Drug: Neratinib|Drug: Neratinib|Drug: Neratinib | Puma Biotechnology, Inc. | Phase 1 | 2010-06-01 | 2012-05-10 |
NCT00958724 | Advanced Malignant Solid Tumors | Drug: treatment with neratinib (HKI-272) + vinorelbine | Puma Biotechnology, Inc. | Phase 1 | 2009-07-01 | 2012-05-10 |
NCT01111825 | Breast Cancer | Drug: Temsirolimus|Drug: Neratinib | Puma Biotechnology, Inc. | Phase 1|Phase 2 | 2010-04-01 | 2016-10-05 |
NCT03065387 | Malignant Neoplasm of Breast|Malignant Neoplasms of Digestive Organs|Malignant Neoplasms of Female Genital Organs|Malignant Neoplasms of Ill-defined Secondary and Unspecified Sites|Malignant Neoplasms of Independent (Primary) Multiple Sites|Malignant Neoplasms of Lip Oral Cavity and Pharynx|Malignant Neoplasms of Mesothelial and Soft Tissue|Malignant Neoplasms of Respiratory and Intrathoracic Organs|Malignant Neoplasms of Thyroid and Other Endocrine Glands|Malignant Neoplasms of Urinary Tract|Neoplasms of Uncertain or Unknown Behavior | Drug: Neratinib|Drug: Everolimus|Drug: Palbociclib|Drug: Trametinib | M.D. Anderson Cancer Center|Pfizer|Puma Biotechnology, Inc. | Phase 1 | 2017-04-01 | 2017-02-28 |
NCT01960023 | Colorectal Cancer | Drug: Cetuximab|Drug: Neratinib | NSABP Foundation Inc | Phase 1|Phase 2 | 2013-10-01 | 2016-05-05 |
NCT01827267 | HER2-mutant Non-Small Cell Lung Cancer | Drug: neratinib|Drug: temsirolimus | Puma Biotechnology, Inc. | Phase 2 | 2013-05-01 | 2017-03-02 |
NCT02236000 | Breast Cancer | Drug: Neratinib|Drug: T-DM1 | NSABP Foundation Inc|Puma Biotechnology, Inc. | Phase 1|Phase 2 | 2014-08-01 | 2017-02-20 |
NCT00781430 | Hepatic Insufficiency | Drug: Neratinib (HKI-272) | Puma Biotechnology, Inc. | Phase 1 | 2009-04-01 | 2012-05-10 |
NCT01956253 | Bladder Cancer | Drug: Neratinib | UNC Lineberger Comprehensive Cancer Center | 2013-07-01 | 2017-03-10 | |
NCT01423123 | Breast Cancer | Drug: Paclitaxel|Biological: trastuzumab|Drug: Neratinib | NSABP Foundation Inc|Pfizer | Phase 1 | 2011-05-01 | 2014-07-07 |
NCT00741260 | Breast Cancer | Drug: Neratinib|Drug: capecitabine | Puma Biotechnology, Inc. | Phase 1|Phase 2 | 2008-12-01 | 2016-06-22 |
NCT02334501 | Healthy | Drug: Lansoprazole|Drug: Neratinib | Puma Biotechnology, Inc. | Phase 1 | 2014-08-01 | 2016-05-09 |
NCT01953926 | Solid Tumors | Drug: Neratinib|Drug: Paclitaxel|Drug: Fulvestrant | Puma Biotechnology, Inc. | Phase 2 | 2013-09-30 | 2017-02-17 |
NCT00864487 | Healthy Subjects | Drug: Neratinib | Puma Biotechnology, Inc. | Phase 1 | 2009-04-01 | 2012-05-10 |
NCT00932464 | Healthy | Drug: Neratinib|Drug: Neratinib | Puma Biotechnology, Inc. | Phase 1 | 2012-08-01 | 2012-05-10 |
NCT02673398 | HER2 Positive Breast Carcinoma|Recurrent Breast Carcinoma|Stage IV Breast Cancer | Other: Comprehensive Geriatric Assessment|Other: Laboratory Biomarker Analysis|Drug: Neratinib|Other: Pharmacological Study | City of Hope Medical Center|National Cancer Institute (NCI)|Puma Biotechnology, Inc. | Phase 2 | 2016-10-01 | 2016-11-30 |
NCT01670877 | Breast Neoplasms | Drug: Neratinib|Drug: Fulvestrant|Drug: Trastuzumab | Washington University School of Medicine | Phase 2 | 2012-12-11 | 2017-02-08 |
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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