抗感染药物临床应用进展课件.ppt

4.抗感染药物临床用药进展米卡芬净Micafungin棘白菌素类，抗菌谱与卡泊芬净相仿蛋白结合率高（99％），t1/2?10-15h主要经肝脏代谢，少部分由肾脏排出2002年日本上市2005年美国上市，适应证及给药方案：造血干细胞移植患者念珠菌感染的预防，50mg/d静滴食道念珠菌病的治疗，150mg/d静滴主要不良反应为恶心、呕吐、血胆红素升高及肝功能异常**ThesearchforanewmedicineThispiperepresentsthelongroadthathastobetraveledtodiscoveranddevelopanewmedicine.Manyprojectshavetobeinitiatedbeforeamedicineisdiscovered.Foreachproject,hundredsofmoleculesfrequentlyhavetobesynthesizedandtestedinbiologicalmodels.Inpreclinicalpharmacology,researchisconductedtounderstandhowsubstancesareabsorbed,convertedandmetabolized,andthenfinallyexcretedfromthebody,allinrelationtotime.Thesafetyofthesubstancemustalsobeminutelyevaluatedinvariousmodels.Thedevelopmentofamedicineisaselectionprocessateachsuccessivephase.Theproblemhereisthatmanysubstancesfallbythewaysideatalatestageofdevelopmentandhavetobediscardedforallkindsofreasons:insufficientactivity,bioavailability,safety,etc.Thepurposeofallthesepreclinicaltestsistopredictwhatmightbeexpectedinclinicalresearch,inotherwordsinthehumanbody.Ideally,itwouldbebetterifthesubstancesthatdonotmeetthecriteriacouldbeidentifiedatanearlystage.Thatwouldsavealotoftimeandmoney.Clinicalpharmacologyandsafetyaccountforaverysubstantialpartofthedevelopmenttime.Thesetrialsinhumansareconductedinvariousphasesandtakefivetosevenyearstocomplete.****4.抗感染药物临床用药进展抗感染药物临床应用进展4.抗感染药物临床用药进展主要内容抗菌药物抗菌药研发存在的问题近年上市或完成Ⅲ期临床试验的新抗菌药新抗菌药开发新思路近3年上市新抗真菌药近3年上市抗病毒药4.抗感染药物临床用药进展主要内容抗菌药物抗菌药研发存在的问题已上市或完成Ⅲ期临床试验的新抗菌药新抗菌药开发新思路近3年上市新抗真菌药近3年上市抗病毒药4.抗感染药物临床用药进展美国批准上市的新抗菌药物

1983-2007ModifiedfromSpellbergB.CID2004;38:127903吉米沙星Gemifloxacin03达托霉素Daptomycin04替利霉素Telithromycin05替吉环素Tigecycline07多立培南Doripenem07Retapamulin抗菌新药研发周期10-12年费用10亿美元ideamedicine1