https://scholars.lib.ntu.edu.tw/handle/123456789/495011
標題: | Second and third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancer | 作者: | BIN-CHI LIAO CHIA-CHI LIN CHIH-HSIN YANG |
公開日期: | 2015 | 出版社: | Lippincott Williams and Wilkins | 卷: | 27 | 期: | 2 | 起(迄)頁: | 94-101 | 來源出版物: | Current Opinion in Oncology | 摘要: | PURPOSE OF REVIEW: The first-generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs), gefitinib and erlotinib, are effective as first-line treatment of advanced nonsmall cell lung cancer (NSCLC) harboring activating EGFR mutations (deletions in exon 19 and exon 21 L858R mutation). EGFR T790?€?M resistance mutation (EGFR) ultimately emerged in most of these patients. The second and third-generation EGFR-TKIs were designed to have more potent inhibition of EGFR and to overcome EGFR. This review describes the recent developments of these novel EGFR-TKIs. RECENT FINDINGS: The second-generation EGFR-TKIs, afatinib and dacomitinib, irreversibly bind to the tyrosine kinase of EGFR and other ErbB-family members. Afatinib has been approved as first-line treatment of advanced NSCLC harboring activating EGFR mutations. Dacomitinib is under development. Third-generation EGFR-TKIs, AZD9291, CO-1686, and HM61713, inhibit both EGFR activating and resistance mutations, while sparing wild-type EGFR. In early-phase studies, these drugs demonstrated promising response rates against tumors with acquired EGFR. SUMMARY: Second-generation EGFR-TKI, afatinib, is available as first-line treatment of advanced NSCLC harboring activating EGFR mutations. Third-generation EGFR-TKIs are under development for tumors harboring acquired EGFR. Copyright ? 2015 Wolters Kluwer Health, Inc. All rights reserved. |
URI: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84922628379&doi=10.1097%2fCCO.0000000000000164&partnerID=40&md5=bdebe30db4d680bf2d74377e20a1b2fb https://scholars.lib.ntu.edu.tw/handle/123456789/495011 |
ISSN: | 1040-8746 | DOI: | 10.1097/CCO.0000000000000164 | SDG/關鍵字: | afatinib; azd 9291; dacomitinib; epidermal growth factor receptor; epidermal growth factor receptor kinase inhibitor; hm 61713; rociletinib; unclassified drug; antineoplastic agent; epidermal growth factor receptor; erlotinib; gefitinib; protein kinase inhibitor; protein tyrosine kinase; quinazoline derivative; advanced cancer; Article; cancer chemotherapy; drug approval; drug protein binding; enzyme inhibition; human; non small cell lung cancer; phase 1 clinical trial (topic); phase 2 clinical trial (topic); phase 3 clinical trial (topic); priority journal; randomized controlled trial (topic); antagonists and inhibitors; Carcinoma, Non-Small-Cell Lung; drug effects; drug resistance; genetics; immunology; Lung Neoplasms; mutation; Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Drug Resistance, Neoplasm; Humans; Lung Neoplasms; Mutation; Protein Kinase Inhibitors; Quinazolines; Receptor Protein-Tyrosine Kinases; Receptor, Epidermal Growth Factor |
顯示於: | 腫瘤醫學研究所 |
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