【摘要】 伊立替康与氟尿嘧啶、亚叶酸联合用于转移性结肠直肠癌的一线治疗,或用于转移性结直肠癌复发和恶化的治疗,其治疗过程中主要的不良反应为骨髓抑制和迟发型腹泻。伊立替康的体内代谢过程复杂,涉及众多药物代谢酶和药物转运蛋白,如羧酸酯酶、细胞色素P450 3A酶、尿苷二磷酸葡醛酰转移酶、ATP-依赖性转运蛋白,且存在药酶多态性现象,药动学和药效学个体差异大。文中主要综述近年来伊立替康体内代谢酶和膜转运蛋白基因多态性对其疗效及毒性作用影响的研究进展。更多还原

【Abstract】 The anticancer agent irinotecan(CPT-11),in combination with 5-fluorouracil and leucovorin,is indicated as a component of first-line therapy for the treatment of metastatic colorectal cancer.It is also used for the treatment of recurrent matastatic colorectal cancer after initial fluorouracil-based therapy.The main adverse effects of irinotecan are myelosuppression and delayed diarrhea.The pharmacokinetics of irinotecan is extremely complex and the individual variation is significant.Irinotecan is subject to extensive metabolism by various polymorphic enzymes,including CES2,members of the uridine diphosphate glucuronosyl transferase(UGT) 1A subfamily,CYP3A and the adenosine-triphosphate(ATP) binding cassette(ABC) transporters.In this article, we reviewed the role of genetic polymorphisms in the main enzymes of inirinotecan metabolism and ABC-transporters.更多还原