肺癌相关酪氨酸激酶抑制剂的药物相互作用

Drug-drug interactions with tyrosine-kinase inhibitors in lung cancer

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。

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 sub-strates 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.