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. 2020 Jun 25;5(26):16076–16084. doi: 10.1021/acsomega.0c01581

Table 2. Summary of the Five Cytochromes (CYPs) Considered in This Work.

CYP brief description references
3A4 It is the most abundant form among the CYP3A subfamily. It has low substrate specificity. Chemical properties of a drug critical to CYP3A4 inactivation include the formation of reactive metabolites by CYP isoenzymes, preponderance of CYP inducers and P-gp substrates/inhibitors, and occurrence of clinically significant PK interactions with coadministered drugs. Mechanism-based inhibition of CYP3A4 causes PK-PD drug–drug interactions that may lead to adverse drug effects (33)
1A2 It is an important metabolizing enzyme in the liver, comprising approximately 13% of all CYP proteins. There are more than 100 substrates reported for CYP1A2 (34)
2C19 It is a clinically important enzyme responsible for the metabolism of several drugs. CYP2C19 is also known to be involved in the detoxification of potential carcinogens or the bioactivation of some environmental procarcinogen(s) to reactive DNA binding metabolites (29)
2C9 It is abundantly expressed and contributes to drug metabolism to the greatest extent. It is the major enzyme responsible for the metabolic clearance of several drugs with a narrow therapeutic index. Thus, interindividual variability in CYP2C9 protein expression and activity may impact the efficacy and safety of drug treatment. CYP2C9 substrates used therapeutically, especially those where drug interactions and effects of genetic polymorphisms may affect treatment outcomes (35)
2D6 It is involved in the hepatic metabolism of many clinically used medications. The CYP2D6 gene is highly polymorphic, and its function is highly variable. People with decreased or no CYP2D6 enzyme activity may be at risk of reduced efficacy and/or adverse effects when taking medications metabolized by CYP2D6 (36)