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A Method to Study the C924T Polymorphism of the Thromboxane A2 Receptor Gene
Published on: April 1, 2019
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The CYP2C9 polymorphism: from enzyme kinetics to clinical dose recommendations
Julia Kirchheiner1, Martina Tsahuridu2, Wafaa Jabrane3
1University of Cologne, Department of Pharmacology, University of Cologne, Gleueler Str. 24, 50931 Koln, Germany. julia.kirchheiner@uk-koeln.de.
Personalized Medicine
|May 26, 2018
Summary
Genetic variations in CYP2C9 (cytochrome P450 2C9) impact drug metabolism, affecting treatments for conditions like diabetes and blood clotting. Genotyping CYP2C9 may personalize drug therapy and reduce adverse events.
Area of Science:
- Pharmacogenomics
- Drug Metabolism
- Enzyme Kinetics
Background:
- CYP2C9 is a key enzyme metabolizing ~10% of clinical drugs.
- Common genetic variants CYP2C9*2 and CYP2C9*3 alter enzyme function.
- Approximately 35% of Caucasians carry at least one of these variants.
Purpose of the Study:
- To review the clinical significance of CYP2C9 polymorphisms.
- To highlight the impact of CYP2C9 variants on drug efficacy and safety.
- To assess the readiness of CYP2C9 genotyping for routine clinical application.
Main Methods:
- Literature review of in vitro and in vivo studies.
- Analysis of clinical pharmacokinetic data.
- Evaluation of studies linking CYP2C9 genotype to drug response and adverse events.
Main Results:
- CYP2C9*2 and *3 variants significantly reduce metabolic activity (70% and 10% of wild-type, respectively).
- Polymorphisms are clinically relevant for oral hypoglycemics, anticoagulants (warfarin, acenocoumarol), NSAIDs, and phenytoin.
- Genotyping can help mitigate risks like bleeding and hypoglycemia and optimize phenytoin therapy.
Conclusions:
- CYP2C9 genotyping is medically important for several drug classes.
- Routine consideration of CYP2C9 genotypes in therapy with specific drugs (e.g., warfarin, phenytoin) is warranted.
- Randomized controlled trials are recommended to validate genotype-guided therapeutic strategies before widespread clinical adoption.
Keywords:
CYP2C9cytochrome P450individualizationpharmacogeneticspharmacogenetics-based dose adjustmentMore Related Videos
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