肺癌相关酪氨酸激酶抑制剂的药物相互作用

doi:10.3760/cma.j.issn.1673422X.2016.12.014

摘要/Abstract

摘要： 近年来，酪氨酸激酶抑制剂（TKI）开始应用于肺癌治疗领域。随着此类新药物的广泛应用，药物相互作用风险也在增加，亟需个体化用药。该类药物均为口服给药，吸收受胃液pH值影响，体内分布广泛、蛋白结合率高，多为转运体ATP结合盒(ABC)B1/G2作用底物，经细胞色素P450（CYP450）同工酶代谢，同时多个TKI为CYP450同工酶及转运体的抑制剂或诱导剂，存在巨大的药物相互作用风险。

关键词: 肺肿瘤, 蛋白酪氨酸激酶类, 蛋白激酶抑制剂, 药代动力学, 药物相互作用

Abstract: The development of the tyrosinekinase inhibitors (TKIs) has led to new treatment options for lung cancer. As this new class of drugs is extensively used, serious drugdrug interactions are in increasing risk, and tailored treatment is urgently needed. All TKIs are given orally, extensively distributed in vivo and highly bound to plasma proteins. A change in stomach pH may affect their absorptions. Most of them are substrates of drug transporters ATPbinding cassette B1/G2 and cytochrome P450 isozymes. At the same time, they often exert an inductive or inhibitory effect on these enzymes. Patients are at substantial risk of having drugdrug interactions during treatment with TKIs in daily clinical practice.

Key words: Lung neoplasms, , Proteintyrosine kinases, Protein kinase inhibitors, Pharmacokinetics, Drug interactions

张帅, 艾斌. 肺癌相关酪氨酸激酶抑制剂的药物相互作用[J]. 国际肿瘤学杂志, 2016, 43(12): 935-939.

ZHANG Shuai, AI Bin. Drugdrug interactions with tyrosinekinase inhibitors in lung cancer[J]. Journal of International Oncology, 2016, 43(12): 935-939.

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