What percentage of the Caucasian population may have poor metabolizer polymorphisms of cytochrome P450 2D6?
What percentage of the Caucasian population may have poor metabolizer polymorphisms of cytochrome P450 2D6?
Most CYP2D6 polymorphisms result in an allele that lacks metabolic activity. However, the prevalence of poor metabolizer phenotypes varies by racial/ethnic group: Asians (∼1%), Caucasians (5–10%), and Africans (0–19%) [58].
How many CYP2D6 variants are there?
The CYP2D6 gene is highly polymorphic; over 100 allelic variants and subvariants have been designated to date by the Pharmacogene Variation Consortium (PharmVar) at www.PharmVar.org (Gaedigk et al., 2018).
Is acetaminophen metabolized by CYP2D6?
It is generally accepted that N-acetyl-p-benzoquinone imine (NAPQI) is the toxic, reactive intermediate whose formation from APAP is mediated by cytochrome P450. We now present evidence which demonstrates that human cytochrome P450 2D6 (CYP2D6) is also involved in the bioactivation of APAP.
What is 2D6 polymorphism?
The polymorphism of the enzyme results in poor, intermediate, efficient or ultrarapid metabolisers (UMs) of CYP2D6 drugs. The polymorphism of CYP2D6 significantly affects the pharmacokinetics of about 50% of the drugs in clinical use, which are CYP2D6 substrates.
What gene is CYP2D6?
Cytochrome P450 2D6 (CYP2D6) is an enzyme that in humans is encoded by the CYP2D6 gene. CYP2D6 is primarily expressed in the liver….
| CYP2D6 enzyme activity for selected alleles | |
|---|---|
| Allele | CYP2D6 activity |
| CYP2D6 duplication | increased |
What genotyping tests are approved by the FDA for the analysis of CYP2D6 variants?
Commercially available CYP2D6 genotyping and sequencing tests. The xTAG CYP2D6 Kit v3 assay is the only CYP2D6 platform approved by the US FDA for in vitro diagnostic testing. The Ion AmpliSeq Pharmacogenomics Research Panel is the only commercial sequencing assay presented in the table.
What happens if you inhibit CYP2D6?
Drugs that inhibit CYP2D6 activity are likely to increase the plasma concentrations of certain medications, and, in some cases, adverse outcomes will occur (see Table 3 below right for a list of known inhibitors).
