Division of Clinical Research, Instituto Nacional de Cancerología (INCan), Mexico City, Mexico.
Med Oncol. 2010 Dec;27(4):1133-43. doi: 10.1007/s12032-009-9349-y. Epub 2009 Nov 10.
Gemcitabine (2',2'-difluoro 2'deoxycytidine, dFdC) is an analog of cytosine with distinctive pharmacological properties and a wide antitumor-activity spectrum. The pharmacological characteristics of gemcitabine are unique because two main classes of genes are essential for its antitumor effects: membrane transporter protein-coding genes, whose products are responsible for drug intracellular uptake, as well as enzyme-coding genes, which catalyze its activation and inactivation. The study of the pharmacogenetics and pharmacoepigenetics of these two gene classes is greatly required to optimize the drug's therapeutic use in cancer. This review aims to provide an update of genetic and epigenetic bases that may account for interindividual variation in therapeutic outcome exhibited by gemcitabine.
吉西他滨（2',2'-二氟脱氧胞苷，dFdC）是胞嘧啶的类似物，具有独特的药理学特性和广泛的抗肿瘤活性谱。吉西他滨的药理学特征是独特的，因为有两类主要的基因对其抗肿瘤作用至关重要：膜转运蛋白编码基因，其产物负责药物的细胞内摄取，以及酶编码基因，其催化药物的激活和失活。研究这两类基因的药物遗传学和药物基因组学对于优化吉西他滨在癌症中的治疗用途非常重要。本综述旨在提供遗传和表观遗传基础的最新信息，这些基础可能解释了吉西他滨治疗结果的个体间差异。
