Alectinib: a novel second generation anaplastic lymphoma kinase (ALK) inhibitor for overcoming clinically-acquired resistance
文献类型：期刊论文
| 作者 | Song, Zilan; Wang, Meining; Zhang, Ao
|
| 刊名 | ACTA PHARMACEUTICA SINICA B
 |
| 出版日期 | 2015-01 |
| 卷号 | 5期号:1页码:34-37 |
| 关键词 | Tyrosine anaplastic lymphoma kinase Alectinib Crizotinib Non-suaall cell lung cancer Resistance ALK mutations EML4-ALK |
| ISSN号 | 2211-3835 |
| DOI | 10.1016/j.apsb.2014.12.007 |
| 文献子类 | Review |
| 英文摘要 | The development of inhibitors for the tyrosine anaplastic lymphoma kinase (ALK) has advanced rapidly, driven by biology and medicinal chemistry. The first generation ALK inhibitor crizotinib was granted US FDA approval with only four years of preclinical and clinical testing. Although this drug offers significant clinical benefit to the ALK-positive patients, resistance has been developed through a variety of mechanisms. In addition to ceritinib, alectinib is another second-generation ALK inhibitor launched in 2014 in Japan. This drug has a unique chemical structure bearing a 5H-benzo[b] carbazol-11(611)-one structural scaffold with an IC50 value of 1.9 nmol/L, and is highly potent against ALK bearing the gatekeeper mutation L1196M with an IC50 of 1.56 nmoL/L. In the clinic, alectinib is highly efficacious in treatment of ALK-positive non-small cell lung cancer (NSCLC), and retains potency to combat crizotinib-resistant ALK mutations L11.96.M, F1174L, R1275Q and C1156Y. (C) 2015 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. All rights reserved. |
| WOS关键词 | CELL LUNG-CANCER ; CH5424802 ; GENE ; CRIZOTINIB ; FUSION ; MET |
| 资助项目 | National Natural Science Foundation of China[81430080] ; National Natural Science Foundation of China[81125021] ; National Natural Science Foundation of China[81373277] ; National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program', China[2012ZX09103-101-035] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5392964 |
| WOS记录号 | WOS:000360008000004 |
| 出版者 | INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276714]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Zhang, Ao |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Synthet Organ & Med Chem Lab, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Song, Zilan,Wang, Meining,Zhang, Ao. Alectinib: a novel second generation anaplastic lymphoma kinase (ALK) inhibitor for overcoming clinically-acquired resistance[J]. ACTA PHARMACEUTICA SINICA B,2015,5(1):34-37. |
| APA | Song, Zilan,Wang, Meining,&Zhang, Ao.(2015).Alectinib: a novel second generation anaplastic lymphoma kinase (ALK) inhibitor for overcoming clinically-acquired resistance.ACTA PHARMACEUTICA SINICA B,5(1),34-37. |
| MLA | Song, Zilan,et al."Alectinib: a novel second generation anaplastic lymphoma kinase (ALK) inhibitor for overcoming clinically-acquired resistance".ACTA PHARMACEUTICA SINICA B 5.1(2015):34-37. |
入库方式： OAI收割
来源：上海药物研究所
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