6533b7d7fe1ef96bd1267a72
RESEARCH PRODUCT
Genetics of the variable expression of CYP3A in humans.
Leszek Wojnowskisubject
PharmacologyGeneticsRegulation of gene expressionPolymorphism GeneticCYP3A4GenomicsOxidoreductases N-DemethylatingBiologyIsozymeGene Expression Regulation EnzymologicVariable ExpressionPharmaceutical PreparationsOrgan SpecificityCytochrome P-450 CYP3ACytochrome P-450 CYP3AHumansPharmacology (medical)PharmacokineticsAryl Hydrocarbon HydroxylasesCYP3A5Hormonedescription
CYP3A isozymes participate in the metabolism of 45-60% of currently used drugs and of a variety of other compounds such as steroid hormones, toxins, and carcinogens. The CYP3A expression status is a major determinant of drug efficacy and safety, and it may also affect an individual's predisposition to certain cancers. The inter- and intraindividual expression of CYP3A is variable because of a complex interplay between genetic and environmental factors. Markers predictive of the individual CYP3A activity could improve therapies with CYP3A substrates by personalised dose adjustments, but their development has been slower than for other drug-metabolizing enzymes. Here we summarize the recent progress in genomics and regulation of CYP3A. The recently described markers of the CYP3A5 and CYP3A7 polymorphisms should facilitate the development of isozyme-specific activity markers for the individual CYP3A isozymes, including CYP3A4.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2004-07-02 | Therapeutic drug monitoring |