Patent NZ-534462-A (NZ)
Title: Test agents for evaluating pharmacological effect of drug, and method and reagents for screening drug having excellent administration effect and/or little side effect from among drugs comprising enzymes, enzyme inhibitors or receptor ligands and/or prodrugs thereof
Inventor: ITO ASUKA
IPC: C12Q1/34
Filed: 2003-02-20
Abstract: It is intended to provide test agents for evaluating the pharmacological effect of a drug such as a drug comprising an enzyme, an enzyme inhibitor or a receptor ligand or its prodrug; and a method of screening a drug having an excellent administration effect and/or little side effect from among drugs comprising enzymes, enzyme inhibitors or receptor ligands and/or prodrugs thereof. Particularly disclosed is a use of any one of the following compounds (a) to (f): (a) a compound which serves as a substrate for an enzyme contained in a medicine to be evaluated or for an enzyme generated from the prodrug contained in the medicine to be evaluated, or a pharmaceutically acceptable salt thereof, wherein the enzyme is streptokinase, streptodornase, hyaluronidase, urokinase, lysozyme, amylase, saccharated pepsin, diastase or pancreatin; (b) a compound which serves as a substrate for a different enzyme capable of exhibiting an alteration in activity by coupling to the effect of the enzyme contained in the medicine to be evaluated or the effect of an enzyme generated from the prodrug contained in the medicine to be evaluated, or a pharmaceutically acceptable salt thereof, wherein the enzyme is trypsin or carboxypeptidase; (c) a compound which serves as a substrate for an enzyme which is directly inhibited by the enzyme inhibitor contained in the medicine to be evaluated or by an enzyme inhibitor generated from the prodrug contained in the medicine to be evaluated, or a pharmaceutically acceptable salt thereof, wherein the enzyme is alpha-glucosidase, pancreatic protease, HMG-CoA reductase, angiotensin converting enzyme, folate reductase, HIV protease, viral reverse transcriptase, DNA polymerase, neuraminidase or DOPA decarboxylase; (d) a compound which serves as a substrate for an enzyme capable of exhibiting an alteration in activity by coupling to the effect of the enzyme inhibitor for the other enzyme, contained in the medicine to be evaluated or the effect of an enzyme inhibitor generated from the prodrug contained in the medicine to be evaluated, or a pharmaceutically acceptable salt thereof, wherein the enzyme is thymidylate synthase or prostaglandin I synthetase; (e) a compound which serves as a substrate for an enzyme capable of exhibiting an alteration in activity by the binding between a receptor and the receptor ligand contained in the medicine to be evaluated or a receptor ligand generated from the prodrug contained in the medicine to be evaluated, or a pharmaceutically acceptable salt thereof, wherein the enzyme is adenylate cyclase; or (f) a labelled form of any one of the compounds (a) to (e); with the proviso that the compound is not a substrate for PHGPx; in the preparation of a diagnostic reagent which is to be used in a method for evaluating the pharmacological effect of a medicine which contains a pharmaceutical agent comprising an enzyme, an enzyme inhibitor, or a receptor ligand, or a prodrug of the pharmaceutical agent.