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随着分子药理学的发展,基因多态性对药物在人体内的分布和代谢过程中发挥着重要的作用。他莫昔芬为美国食品药品监督管理局(FDA)规定的雌激素受体阳性的乳腺癌患者内分泌治疗的金标准药,其在乳腺癌患者体内的疗效存在较大的个体差异。细胞色素P450(CYP450)代谢酶和常见转运体的基因多态性影响了他莫昔芬在乳腺癌患者体内的药代动力学/药效学。本文就CYP450代谢酶和常见转运体的基因多态性对他莫昔芬的药代动力学/药效学影响展开综述,为他莫昔芬的临床个体化治疗提供一定的参考依据。
With the development of molecular pharmacology, genetic polymorphisms play an important role in the distribution and metabolism of drugs in the human body. Tamoxifen is the gold standard drug for endocrine therapy of estrogen receptor positive breast cancer patients regulated by the U.S. Food and Drug Administration (FDA), and there is a large individual difference in the efficacy of breast cancer patients. Genetic polymorphisms of cytochrome P450 (CYP450) metabolizing enzymes and common transporters influence the pharmacokinetics / pharmacodynamics of tamoxifen in breast cancer patients. In this review, we reviewed the pharmacokinetics / pharmacodynamic effects of CYP450 metabolic enzymes and common transporters on the tamoxifen pharmacokinetics / pharmacodynamics, and provided some references for the clinical individualized treatment of tamoxifen.