CYP2D6基因多态性对他莫昔芬及托瑞米芬代谢和疗效影响的研究进展

他莫昔芬和托瑞米芬均为选择性的雌激素受体调节剂,通过竞争性结合雌激素受体发挥抗癌作用,是绝经前乳腺癌最常用的辅助内分泌治疗药物,能够显著降低乳腺癌患者的复发和死亡风险。多项研究发现CYP2D6*10基因的突变会影响他莫昔芬的代谢导致预后不良。而托瑞米芬的代谢受CYP2D6基因多态性的影响较小,治疗乳腺癌的疗效与他莫昔芬相当,甚至优于他莫昔芬。本文就CYP2D6基因多态性与两种内分泌药物代谢和疗效的相关性研究作系统阐述。

Research progress of CYP2D6 gene polymorphism on the metabolism and efficacy of tamoxifen and toremifene

Tamoxifen and toremifene are selective estrogen receptor modulators.Both play a role in competitively binding estrogen receptors.They are the most commonly used adjuvant endocrine therapy for premenopausal breast cancer and can significantly reduce the risk of recurrence and death in breast cancer patients.A number of studies have found that mutations in CYP2D6*10 gene affect the metabolism of tamoxifen leading to a poor prognosis.The metabolism of toremifene is less affected by the CYP2D6 polymorphism.The efficacy of toremifene in the treatment of breast cancer is comparable to tamoxifen,and even better than tamoxifen.This article systematically describes the relationship between CYP2D6 polymorphism and the metabolism and efficacy of two endocrine drugs.