植物学及园艺学英文版 botany and horticulture 89

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1、MedicinalChemistry&DrugDiscoveryDr.PeterWipfDepartmentofChemistryUniversityofPittsburghhttp://ccc.chem.pitt.edu/wipf/index.htmlhttp://ccc.chem.pitt.edu/wipf/Courses.html•Surveyofcurrentdrugs•Drugdiscoverychallenges•Methodstoidentifynewleads•Casestudiesfromindustry•Forward

2、chemicalgenetics-reversepharmacologyMedicinalChemistryThesciencethatdealswiththediscoveryordesignofnewtherapeuticagentsandtheirdevelopmentintousefulmedicines.Itinvolves:SynthesisStructure-ActivityRelationships(SAR)ReceptorinteractionsAbsorption,distribution,metabolism,ande

3、xcretion(ADME)2003BlockbustersattheDrugstore(US/Worldwide;outof~$500b)Lipitor(Pfizer)cholesterol$6.8/10.3billion(66%)Zocor(Merck)cholesterol$4.4/6.1billion(72%)Zyprexa(EliLilly)antipsychotic$3.2/4.8billion(72%)Norvasc(Pfizer)bloodpressure$2.2/4.5billion(40%)Procrit(J&J)ane

4、mia$3.3/4.0billion(83%)Prevacid(TAP)ulcers$4.0/4.0billion(100%)Nexium(AstraZeneca)ulcers$3.1/3.8billion(82%)Plavix(BMS-Sanofi)bloodthinner$2.2/3.7billion(59%)Seretide(GSK)asthma$2.3/3.7billion(62%)Zoloft(Pfizer)depression$2.9/3.4billion(85%)Epogen(Amgen)anemia$3.1/?billion

5、(?%)Celebrex(Pfizer)arthritis$2.6/?billion(?%)Source:IMSHealth,March2004“BigPharma”DrugDiscoveryinthe21stCenturyTheProblem:Thepharmaceuticalindustryisshortofnewdrugs.Inthe2ndpartofthe20thcentury,about50-60newdrugs(NCEs)wereapprovedbytheFDAeveryyear.Incontrast,in2002,ahisto

6、ricallowof18NCEswereapproved(in2001,24NCEs,in2000,27NCEs,in2003,21NCEs).Conversely,researchcostsforanewdrugareestimatedtobeinthe$1-1.5Bi.range.Consideringallhigh-profilefailuresinrecentdrugdiscovery,thisfigureisunlikelytodropsubstantially.Source:WallStreetJ.11/21/2003“…glo

7、omaroundthepharmaceuticalscompany..”Source:WallStreetJ.2/24/2004Wallstreet(andcompanies)arelookingforascapegoat..”DrugIndustry'sBigPushIntoTechnologyFallsShort.TestingMachinesWereBuiltToStreamlineResearch--ButMayBeStiflingIt“Adecadeago,pharmaceuticalcompaniesannouncedarevo

8、lutionarynewwayoffindingdrugs.Insteadofrelyingonscientists'hunchesaboutwhatchemicalstoexp