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。
Antibiotic
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).