In Vitro Cytochrome P450 2C9 (CYP2C9) Intrinsic Clearance Measurement Service
Cytochrome P450 2C9 (CYP2C9) is a cytochrome P450 enzyme that is responsible for metabolizing a wide range of drugs, including warfarin, phenytoin, and tolbutamide. CYP2C9 phenotyping assay can provide valuable information on the involvement of CYP2C19 in drug metabolism. Results from CYP2C9 phenotyping also inform clinical decision-making, such as selecting appropriate drug therapies, adjusting drug dosages, and predicting drug-drug interactions, thus improving treatment outcomes and minimizing the risk of adverse drug reactions.
To assess if a test compound is a substrate for the CYP2C9 enzyme, Creative Biolabs is committed to offering a CYP2C9 intrinsic clearance assay for the understanding metabolism of the compound by the enzyme. This assay is typically performed using human liver microsomes or recombinant CYP2C9 enzyme in vitro.
Our Approach to CYP2C9 Assay Service
To assess if a test compound is a substrate for the CYP2C9 enzyme, two in vitro experiments are available at our lab:
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Recombinant Human CYP2C9 Enzyme
A CYP2C9 intrinsic clearance assay commonly uses recombinant human CYP2C9 enzyme to assess if the CYP2C9 enzyme plays a role in the metabolism of a test compound. This assay involves incubating the test drug with recombinant CYP2C9 enzyme in the presence of co-factors necessary for enzyme activity. The metabolism of the test drug by the CYP2C9 enzyme is then monitored, and the remaining of the test compound or the formation of metabolites is quantified using HPLC-MS/MS.
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Chemical Inhibition Assay
Human liver microsomes contain a full complement of drug-metabolizing enzymes including CYP2C9. A CYP phenotyping assay using human liver microsomes can provide valuable insights into the activity of the CYP enzyme in the metabolism of specific drugs. In the absence and presence of CYP inhibitors, the test drug incubates with human liver microsomes and specific cofactors. By comparing the metabolic activity of CYP with and without specific inhibitors, the assay can help determine the contribution of CYP enzymes to the overall biotransformation of the drug.
Our Capabilities
At Creative Biolabs, our CYP2C9 phenotyping service offers a comprehensive intrinsic clearance analysis utilizing cutting-edge techniques to evaluate the activity of the CYP2C9 enzyme in drug metabolism. By utilizing recombinant enzyme technology, we are able to accurately determine the interaction between the test drug and the CYP2C9 enzyme, providing essential information for drug development and personalized medicine. Additionally, our CYP2C9 intrinsic clearance assays using human liver microsomes allow us to provide valuable data to support the development and safe use of pharmaceuticals. With our expertise in CYP phenotyping assays and other ADME services, we offer tailored solutions to provide valuable insights into the intrinsic clearance and metabolic capabilities of CYP2C9.
Support Data
Data 1: The experiment was performed to determine whether CRV43 was a substrate metabolized by recombinant human CYP enzymes. The results indicate that CYP3A4 plays the primary role in the metabolism of CRV431.
Fig.1 Metabolism of CRV43 by a panel of human rCYP enzymes.1,2
References
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Trepanier, Daniel J., Daren R. Ure, and Robert T. Foster. "In vitro phase I metabolism of CRV431, a novel oral drug candidate for chronic hepatitis B." Pharmaceutics 9.4 (2017): 51.
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Distributed under Open Access license CC BY 4.0, without modification.
For Research Use Only | Not For Clinical Use
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