小分子靶向抗肿瘤药物耐药机制与应对策略  

Mechanism of Drug Resistance and Coping Strategies for Small Molecule Targeted Anticancer Drugs

作　　者：廖敏 强晓妍 盛泽娟 彭鹏 LIAO Min;QIANG Xiaoyan;SHENG Zejuan;PENG Peng(Trans Thera Sciences(Nanjing),Inc.,Nanjing,210032,China)

机构地区：[1]药捷安康(南京)科技股份有限公司,江苏南京210032

出　　处：《药学进展》2023年第9期693-705,共13页Progress in Pharmaceutical Sciences

摘　　要：癌症是危害人类健康的重要因素,并已经成为全球第二大致死病因。随着小分子靶向抗癌药物的出现与广泛应用,癌症的治愈率与患者的生存期均显著提高。但肿瘤耐药问题随之而来,大部分小分子靶向抗肿瘤药物在应用一段时间后会出现不同程度的耐药现象。深入研究小分子靶向抗癌药物的耐药机制是寻找克服肿瘤耐药策略的必经之路。通过对小分子靶向抗癌药物常见的一些耐药机制进行总结,并提出了一些相应的克服肿瘤耐药的策略,以期为相关药物研发提供一定的参考。As the second leading cause of death worldwide,cancer is one of the major public health problems.The emergence and extensive utilization of small molecule targeted anti-cancer drugs have led to substantial improvements in the cure rate of cancer and the survival of patients.However,the subsequent problem of drug resistance arises,with a significant proportion of small molecule targeted anti-cancer drugs showing varying levels of resistance after a duration of administration.Investigating the mechanism underlying drug resistance is essential for identifying effective strategies to overcome the resistance in small molecule targeted anti-cancer therapies.This review provides a comprehensive summary of the prevailing drug resistance mechanisms reported in small molecule targeted anticancer therapies.Additionally,strategies to overcome drug resistance are proposed,thereby offering valuable references for further drug development efforts.

关 键 词：小分子 抗癌药物 靶向治疗 耐药机制 

分 类 号：R914[医药卫生—药物化学] R979.1[医药卫生—药学]