Tan Sing-Huang, Lee Soo-Chin, Goh Boon-Cher, Wong John
Department of Hematology-Oncology, National University of Singapore, National University Health System, Singapore, Singapore.
Clin Cancer Res. 2008 Dec 15;14(24):8027-41. doi: 10.1158/1078-0432.CCR-08-0993.
Interindividual and interethnic variability of drug pharmacokinetics and pharmacodynamics may be contributed by commonly occurring genetic polymorphisms of drug-metabolizing enzymes and transporters. Polymorphisms of CYP2D6 in particular have been associated with effects on tamoxifen disposition and clinical efficacy, with interethnic differences in distribution of functional alleles that affect metabolizer phenotype. Other tamoxifen-related genetic variants of CYP3A4, CYP3A5, and sulfotransferase1A1 (SULT1A1) are also briefly reviewed here. Polymorphisms of CYP19A1 (aromatase gene) have been reported to correlate with clinical outcomes from aromatase inhibitors in small studies but require further confirmation. Many studies on chemotherapy are based on hypothesis-generating association studies and need to be validated through larger-scale cooperative group studies. For anthracyclines, polymorphisms in genes such as carbonyl reductase 3 (CBR3), ATP-binding cassette subfamily B, member 1 (ABCB1), glutathione-related transporter genes, and oxidative stress-related genes have been reported to correlate with clinical outcomes. The pharmacogenetics of taxanes has been extensively investigated, but associations of genetic polymorphisms in drug-metabolizing enzymes and transporters reported in earlier small studies have not been validated in a recent large clinical trial. Allelic variants associated with gemcitabine, capecitabine/5-fluorouracil, vinorelbine, and platinum disposition are reviewed. No pharmacogenetic studies have been published for targeted agents thus far, although several potential candidate genes warrant investigation. Future pharmacogenetic studies will need to focus on integration of multiple drug pathways to allow a more comprehensive analysis of genetic factors influencing drug efficacy and toxicity.
药物代谢酶和转运体常见的基因多态性可能导致个体间和种族间药物药代动力学和药效学的差异。特别是CYP2D6的多态性与他莫昔芬的处置和临床疗效有关,影响代谢表型的功能性等位基因分布存在种族差异。本文还简要综述了CYP3A4、CYP3A5和磺基转移酶1A1(SULT1A1)其他与他莫昔芬相关的基因变异。在小型研究中,CYP19A1(芳香化酶基因)的多态性据报道与芳香化酶抑制剂的临床结果相关,但需要进一步证实。许多关于化疗的研究基于产生假设的关联研究,需要通过大规模合作组研究进行验证。对于蒽环类药物,据报道羰基还原酶3(CBR3)、ATP结合盒亚家族B成员1(ABCB1)、谷胱甘肽相关转运体基因和氧化应激相关基因等基因的多态性与临床结果相关。紫杉烷类的药物遗传学已得到广泛研究,但早期小型研究报道的药物代谢酶和转运体基因多态性与临床结果的关联在最近的大型临床试验中尚未得到验证。本文综述了与吉西他滨、卡培他滨/5-氟尿嘧啶、长春瑞滨和铂处置相关的等位基因变异。尽管有几个潜在的候选基因值得研究,但迄今为止尚未发表关于靶向药物的药物遗传学研究。未来的药物遗传学研究需要专注于整合多种药物途径,以便更全面地分析影响药物疗效和毒性的遗传因素。