Michael Michael, Doherty Margaret M
Peter MacCallum Cancer Centre, Division of Haematology and Medical Oncology, Locked Bag 1, A'Beckett Street, Victoria, 8006, Australia.
Expert Opin Drug Metab Toxicol. 2007 Dec;3(6):783-803. doi: 10.1517/17425255.3.6.783.
Drug-metabolising enzymes (DMEs) are present in tumours and are capable of biotransforming a variety of antineoplastics. Tumoural drug metabolism is both a potential mechanism of resistance and a means of achieving optimal therapy. This review addresses the classes of DMEs, their cytotoxic substrates and distribution in specific malignancies. The limitations of preclinical and clinical studies are highlighted. Their role in predicting therapeutic response, the activation of prodrugs and the potential for their modulation for gain is also addressed. The contribution of tumoural DMEs to cancer therapy can only be ascertained through large prospective studies and supported by new technologies. Only then can efforts be concentrated in the design of better prodrugs or combination therapy to optimise individual therapy.
药物代谢酶（DMEs）存在于肿瘤中，能够对多种抗肿瘤药物进行生物转化。肿瘤药物代谢既是耐药的潜在机制，也是实现最佳治疗的一种手段。本综述阐述了药物代谢酶的类别、它们的细胞毒性底物以及在特定恶性肿瘤中的分布情况。同时强调了临床前和临床研究的局限性。还探讨了它们在预测治疗反应、前体药物激活以及调节以获得疗效方面的作用。肿瘤药物代谢酶对癌症治疗的贡献只能通过大型前瞻性研究来确定，并得到新技术的支持。只有这样，才能将精力集中在设计更好的前体药物或联合治疗方案上，以优化个体化治疗。
