CYP2D6代谢酶是细胞色素P450家族中的成员之一,是参与Ⅰ相代谢和众多内源性物质和不同药物消除的酶。虽然它在肝脏中的含量大约只占肝脏总量的2%,但在临床上却参与了25%以上的常用药物的代谢活动。在所有参与药物代谢的细胞色素P450基因家族中,CYP2D6是唯一不能被诱导的酶,这种酶具有广泛的多态性,这种多态性对酶的药物代谢功能具有重要影响,CYP2D6的这种多态性和药物代谢功能所表现的对个体活性的差异,在遗传药理学上具有重要意义。本文从CYP2D6基因多态性和它对药物代谢的影响这两方面进行了阐述。
CYP2D6 is a member of cytochrome P450 gene family-a group of enzymes that is responsible for phase I metabolism and elimination of numerous endogenous substrates and a diverse array of drugs.It is now thought to be involved in the metabolism of up to 25% of the drugs that are in common use in the clinic,despite its low hepatic content(about 2 %).Among the drug-metabolizing cytochrome P450s,CYP2D6 is the only non-inducible enzyme and is highly polymorphic,which results in a large contribution of genetic variation to its inter-individual variation in enzyme activity and is an enzyme of great historical importance for pharmacogenetics.Here we summarize the polymorphism of CYP2D6 gene and their influence to drug metabolism.