Whilst CYP2D6 is involved in the oxidation of a wide range of substrates of all the CYPs, there is considerable variability in its expression in the liver. The gene is located near two cytochrome P450 pseudogenes on chromosome 22q13.1. Alternatively spliced transcript variants encoding different ...
Table 1: Class list of major CYP2D6 isoenzyme substrates [ 3, 4]. In our previous work [8], we tried to create a complete genotyping method for the simultaneous analysis of CYP3A4, CYP3A5, CYP2C9, CYP2C19, and CYP2D6 SNPs. The genotyping of the CYP2D6 gene was difficult due to ...
Drugs metabolized by CYP2D6 arecalled CYP2D6 substrates (see Table 2 at right). Keep in mind that many drugs are metabolized by more than one CYP450 enzyme, and CYP2D6 may represent only one pathway. For example, most tricyclic antidepressants undergo CYP2D6 metabolism, but other CYP450 enzym...
Effect of gender, sex hormones, time variables and physiological urinary pH on apparent CYP2D6 activity as assessed by metabolic ratios of marker substrates. Pharmacogenetics. 2000;10(5):425–438. doi:10.1097/00008571- 200007000-00006 31. Kashuba ADM, Nafziger AN, Kearns GL, et al. ...
A total of 72 interactions were monitored using proluciferin probe substrates. The results showed that the co-expression of UGTs had a significant effect on CYP activity in the majority of cases (88%), with both positive (58%) and negative (30%) effects observed. Conversely, the effect of...
Increased expression of this allele has been associated with some substrates, but its effect on tamoxifen metabolism is not well understood. Gene conversion—a mechanism of mutation transfer between the pseudogene and the gene—may also fail to be analyzed by a given platform. Gene conversions may...
gene conversion (CYP2D8).13 The CYP2D locus also contains GC-rich regions, and two, Alu-rich, 2.8-kb repeated regions (REP6 and REP7) that are substrates for a wide variety of common structural variations of CYP2D6, including copy-number variations (CNVs), gene conversions, rearrangements...
It is of potential clinical importance to be able to identify individuals who have altered pharmacokinetics for CYP2D6 substrates as appropriate dosage strategies for these drugs can be adopted and ADRs can be avoided. The principle that a good therapy is based on a good diagnostic determines, ...
Among the long list of drugs and substrates are many antidepressants and antipsychotics, pain medications such as codeine and tramadol, the estrogen receptor antagonist tamoxifen, and also drugs of abuse1–3. CYP2D6 activity varies widely in most populations with the potential to affect the ability...
Table of Substrates, Inhibitors and Inducers. Available online: https://www.fda.gov/drugs/drug-interactions-labeling/drug-development-and-drug-interactions-table-substrates-inhibitors-and-inducers (accessed on 16 September 2022). Shin, J.; Hills, N.K.; Finley, P.R. Combining Antidepressants with...