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The cytochrome P450 (CYP) enzymes are the major enzymes involved in drug metabolism. Most drugs are substrates of one or more of CYP enzymes. Among the many different isoforms of CYP, a few are particularlly important, including 1A2, 2C9, 2C19, 2D6, and 3A4, contributing to 7%, 9%, 6%, 21%, and 48% of drug metabolism, respectively. Together they account for more than 90% of drug metabolism.

If a drug candidate inhibits the activity of one of the CYPs listed above, it will slow the metabolism and clearance of drugs which are substrates of the inhibited CYP, leading to drug-drug interaction. Therefore, it is important to screen compounds for CYP inhibition to eliminate the potential risk for drug-drug interactions.

Drumetix determines the inhibition of the activity of a CYP isoform by incubating a selective marker substrate for the CYP in human liver microsomes with or without the addition of a drug candidate as a potential inhibitor.

After incubation, the concentration of the marker substrate metabolite is analyzed by LC-MS/MS. Percent inhibition by the drug candidate can be calculated by comparing the concentration of the metabolite in the incubation with the addition of the drug candidate to the one without the addition of the drug candidate. To determine the IC50 of the drug candidate, incubations with the addition of the drug candidate at different concentration levels will be performed.

Drumetix provides inhibition assay for CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Known inhibitors will be used as positive controls in our CYP inhibition assay.