METHOD FOR TESTING CAPABILITY OF IRREVERSIBLY INHIBITING ENZYME HAVING MEDICINE-METABOLIZING FUNCTION

摘要

PROBLEM TO BE SOLVED: To provide a method for testing the capability of irreversibly inhibiting an enzyme having a medicine-metabolizing function of a substance easily and in a good accuracy.;SOLUTION: This method for authorizing the capability of irreversibly inhibiting an enzyme having a medicine-metabolizing function is provided by performing (1) a process of deciding mixed system enzymes (a main group of the enzymes) consisting of ≥2 kinds of mammalian-originated medicine-metabolizing enzymes, mixed system index substrates (a main group of the substrates) consisting of ≥2 index substrates capable of becoming an index corresponding to each of the enzymes and a reaction liquid containing a mixed system solvent suitable for both of the main group of the substrates and main group of enzymes, (2) a process of forming metabolized materials as mixed system metabolized materials (a main group of metabolized materials) by reacting the main group of the enzymes with the main group of the substrates in the reaction liquid by adding the main group of the substrates to a reaction system after making the main group of the enzymes in contact with a test substance, (3) a process of measuring the amounts of production of the main group of the metabolites in the previous process by using a HPLC tandem type mass spectrometer, and (4) a process of evaluating the presence or absence of irreversible inhibitory function, etc., under a specific condition, based on the measured amounts of production or index values in the previous process.;COPYRIGHT: (C)2008,JPO&INPIT