非小细胞肺癌患者厄洛替尼个体化给药研究进展  

Research progress in individualized administration of erlotinib for non-small cell lung cancer

作　　者：肖博文 姚敦武[1] 付滢舟[1] 曹丽芝[1] 向大雄[2] 廖德华[1] XIAO Bo-wen;YAO Dun-wu;FU Ying-zhou;CAO Li-zhi;XIANG Da-xiong;LIAO De-hua(Department of Pharmacy, Hunan Cancer Hospital, Changsha 410013;Department of Pharmacy, Second Xiangya Hospital, Central South University, Changsha 410011)

机构地区：[1]湖南省肿瘤医院药学部,长沙410013 [2]中南大学湘雅二医院药学部,长沙410011

出　　处：《中南药学》2018年第11期1556-1560,共5页Central South Pharmacy

基　　金：国家自然科学基金青年基金(No.81603206);湖南省卫计委科研项目(No.B20180252);湖南省药学会基金课题(No.hn2017005)

摘　　要：治疗药物监测(TDM)作为药学监护服务的重要手段,目前广泛地应用于临床。TDM通过测定患者生物样本中的药物浓度,结合药代动力学原理指导个体化给药,以减少不良反应、提高药物疗效。被监测的药物通常具有治疗指数低、药物浓度个体间差异大、易发生药物相互作用等特点。厄洛替尼作为第一代小分子酪氨酸激酶抑制剂(TKI),对于具有表皮生长因子受体(EGFR)敏感突变的非小细胞肺癌(NSCLC)患者具有显著的靶向抗肿瘤作用。但在标准给药剂量下,患者之间具有显著的药代动力学差异,血药浓度可相差3～5倍,导致患者之间的疗效不一,有些患者甚至出现严重的不良反应。为此,对使用厄洛替尼的NSCLC患者开展个体化给药很有必要。本文就厄洛替尼的作用机制、个体差异大的原因及TDM进行了综述。As a typical means of pharmacy service, therapeutic drug monitoring(TDM) is widely used in clinical practice. By determining the concentration of biological samples and combining pharmacokinetic principles, TDM helps achieve individualized administration, reduce adverse events and improve drug efficacy. Low therapeutic indexes, large individualized differences and easy drug interactions are the most common characteristics of monitored drugs. Erlotinib is the first generation of orally administered small-molecule tyrosine kinase inhibitor(TKI), which is approved as the first-line treatment for advanced non-small cell lung cancer(NSCLC) for patients with activating epidermal growth factor receptor(EGFR) mutations. Increasing evidence showed the steady state concentration of erlotinib with large interindividual variability in systemic exposure. Pharmacokinetic variability of erlotinib is always accompanied with the variability observed in both response and toxicity. It is important to conduct TDM for NSCLC patients who receive erlotinib at a fixed dose. This review summarizes conduct findings of and trends for the TDM of eroltinib for NSCLC.

关 键 词：非小细胞肺癌 厄洛替尼 表皮生长因子受体 治疗药物监测 

分 类 号：R273[医药卫生—中西医结合]