中文名称德拉沙星葡甲胺盐中文同义词德拉沙星N-甲基葡萄糖胺盐;德拉沙星葡甲胺盐;地拉沙星葡甲胺;德拉沙星葡甲胺;DELAFLOXACIN葡甲胺盐;德拉沙星葡甲陂;(2R,3R,4R,5S)-6-(甲氨基)己烷-1,2,3,4,5-戊醇-1-(6-氨基-3,5-二氟吡啶-2-基)-8-氯-6-氟-7-(3-羟基氮杂丁-1-基)-4-氧基-1,4-二氢喹啉-3-羧酸酯;德拉沙星葡胺英文名称ABT-492MegluMine英文同义词100850;ABT492meglumine(Delafloxacinmeglumine);Delafloxacinmeglumine(ABT492meglumine;(2R,3R,4R,5S)-2,3,4,5-tetrahydroxy-6-(MethylaMino)hexyl1-(6-aMino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylate;ABT492MegluMine;ABT492MegluMine;ABT-492MegluMine;Delafloxacin(MegluMine)CAS号352458-37-8分子式C25H29ClF3N5O9分子量635.98EINECS号相关类别抑制剂;原料药;常规产品;原料药及中间体;医药原料;APIMol文件352458-37-8.mol结构式德拉沙星葡甲胺盐性质储存条件underinertgas(nitrogenorArgon)at2–8°C溶解度溶于二甲基亚砜形态粉末颜色米白色至黄色德拉沙星葡甲胺盐用途与合成方法简介德拉沙星葡甲胺(delafloxacinmeglumine)由日本湧永制药株式会社(WakunagaPharmaceuticalCo.Ltd.)研制,1996年授予美国RIB-X制药公司全球独家开发权,由该公司旗下Melinta生物制药公司全权负责研发、上市、生产和销售。美国参议院为激励抗菌药物的研发,于2012年6月26日审议通过美国抗菌药物研发法案,即《食品药品管理局安全与创新法案》(FDASIA)。2014年尚处于Ⅲ期临床试验的德拉沙星葡甲胺符合美国食品药品管理局(FDA)制定的"合格的抗感染药品"(QIDP)认证条件,从而获得优先审评待遇,于2017年6月19日获准上市,商品名为Baxdela。药理作用德拉沙星葡甲胺是一种新型的氟喹诺酮类广谱抗菌药,具有阴离子特性,在酸性条件下具有较好的抗菌活性。通过抑制细菌DNA的复制过程,从而达到杀菌的作用。用途德拉沙星葡甲胺盐对革兰氏阳性菌,革兰氏阴性菌和厌氧菌都具有较好的抗菌活性,可用于治疗急性细菌性皮肤和皮肤结构感染。其具有较好的安全性和耐受性,没有明显的心脏QT间期延长和光毒性。生物活性Delafloxacinmeglumine(ABT492meglumine;RX-3341meglumine;WQ-3034meglumine)是一种广谱氟喹诺酮类抗生素。Delafloxacin具有广泛的活性,对耐药性的金黄色葡萄球菌,肺炎链球菌和肺炎克雷伯菌都有效。靶点Antibiotic体内研究Delafloxacin(thetotaldailydosesvaryfrom0.156to640mgChemicalbook/kg/24h,subcutaneousinjection)ishighlyeffectiveagainstS.aureus.Againstallfourstrainsareobservedadecreaseof1.5to2.2log10CFUinorganismburdenfromuntreatedcontrolsateventhelowestdosestudied,andfortwostrains(MW2andR2527)thereisnetbactericidalactivityatthelowestdose.Atthemaximaldosesstudied,thereisa>4-log10killfrominitialburdenforallS.aureusstrains.Delafloxacin(2.5,10,40,and160mg/kg;subcutaneousinjection,24h)hasmoderateterminaleliminationhalf-life(t1/2=0.68h,0.79h,0.69hand1.0hfor2.5mg/kg,10mg/kg,40mg/kg,and160mg/kg,respectively).AnimalModel:Micewithaneutropenicmurinelunginfectionmodel(fourS.aureus,fourS.pneumoniae,andfourK.pneumoniaestrains)Dosage:Thetotaldailydosesvaryfrom0.156to640mg/kg/24hAdministration:0.03to160mg/kgareadministeredevery6h(q6h)toinfectedmicebysubcutaneousinjectionResult:InhibitedS.aureusstrainsATCC29213,ATCC33591,MW2,R2527withMICsof0.008,0.008,0.004,and0.004mg/L,respectively.InhibitedS.pneumoniaestrainsATCC10813,ATCC49619,145,and1329withMICsof0.03,0.125,0.016,and0.016mg/L,respectively.InhibitedK.pneumoniastrainsATCC43816,4105,4110,and81-1260AwithMICsof0.06,1,0.5,and0.06mg/L,respectively.AnimalModel:NeutropenicmiceDosage:2.5,10,40,and160mg/kg;0.2mLAdministration:Subcutaneousinjection;24hResult:Themaximumdrugconcentrations(Cmax)concentrationsrangedfrom2to71mg/L.AUC0-∞valuesrangedfrom2.8to152mg•h/Landwerelinearacrossthe2.5-to160-mgdosingrange.Theeliminationhalf-life(t1/2)rangedfrom0.7to1h. |