352458-37-8 德拉沙星葡甲胺盐

• 简介 德拉沙星葡甲胺(delafloxacin meglumine)由日本湧永制药株式会社(Wakunaga Pharmaceutical Co. 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。
• 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 Delafloxacin meglumine (ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine) 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 (the total daily doses vary from 0.156 to 640 mg/kg/24 h, subcutaneous injection) is highly effective against S. aureus . Against all four strains are observed a decrease of 1.5 to 2.2 log 10 CFU in organism burden from untreated controls at even the lowest dose studied, and for two strains (MW2 and R2527) there is net bactericidal activity at the lowest dose. At the maximal doses studied, there is a >4-log 10 kill from initial burden for all S. aureus strains. Delafloxacin (2.5, 10, 40, and 160 mg/kg; subcutaneous injection, 24 h) has moderate terminal elimination half-life (t 1/2 =0.68 h, 0.79 h, 0.69 h and 1.0 h for 2.5 mg/kg, 10 mg/kg, 40 mg/kg, and 160 mg/kg, respectively). Animal Model: Mice with a neutropenic murine lung infection model (four S. aureus , four S. pneumoniae , and four K. pneumoniae strains) Dosage: The total daily doses vary from 0.156 to 640 mg/kg/24 h Administration: 0.03 to 160 mg/kg are administered every 6 h (q6h) to infected mice by subcutaneous injection Result: Inhibited S. aureus strains ATCC 29213, ATCC 33591, MW2, R2527 with MICs of 0.008, 0.008, 0.004, and 0.004 mg/L, respectively. Inhibited S. pneumoniae strains ATCC 10813, ATCC 49619, 145, and 1329 with MICs of 0.03, 0.125, 0.016, and 0.016 mg/L, respectively. Inhibited K. pneumonia strains ATCC 43816, 4105, 4110, and 81-1260A with MICs of 0.06, 1, 0.5, and 0.06 mg/L, respectively. Animal Model: Neutropenic mice Dosage: 2.5, 10, 40, and 160 mg/kg; 0.2 mL Administration: Subcutaneous injection; 24 h Result: The maximum drug concentrations (C max ) concentrations ranged from 2 to 71 mg/L. AUC 0-∞ values ranged from 2.8 to 152 mg•h/L and were linear across the 2.5- to 160-mg dosing range. The elimination half-life (t 1/2 ) ranged from 0.7 to 1 h.

医药