CYP enzymes are responsible for metabolizing a vast majority of drugs in the human body. These enzymes, found primarily in the liver, can be the source of drug–drug interactions. In particular, compounds with a single enzyme elimination pathway face a high victim potential in vivo. Hence, studies for the identification of enzymes associated with a compound’s metabolism are recommended.
Our CYP phenotyping elucidates the involvement of up to 21 CYP isoforms in the metabolism of your test compound. Therefore, we incubate the test compounds with recombinant human CYP isoenzymes in the presence and absence of NADPH and determine the difference in depletion. In parallel, we monitor the formation of known metabolites and, based on both observations, specify the involvement of the respective isoenzyme. Subsequently, the fraction metabolized by the identified enzymes can be determined. To this end, we incubate human hepatocytes with CYP-isoform-specific inhibitors. The clearance of the test item in these pretreated hepatocytes is determined, and the fraction metabolized by the respective enzyme can be calculated.
Our experienced team works closely with you to optimize your CYP phenotyping studies, provides expert data interpretation, and offers strategic recommendations for successfully advancing your drug discovery project. With our excellent capabilities and deep expertise, we are your trusted partner for CYP phenotyping studies.