352458-37-8
352458-37-8 結(jié)構(gòu)式
基本信息
德拉沙星葡甲胺
地拉沙星葡甲胺
德拉沙星葡甲胺鹽
352458-37-8
德拉沙星N-甲基葡萄糖胺鹽
DELAFLOXACIN葡甲胺鹽
ABT492 MegluMine
ABT 492 MegluMine
ABT-492 MegluMine
RX-3341 meglumine
ABT-491 MegluMine
WQ-3034 meglumine)
Delafloxcain meglumine
Delafloxacin Mcglumine
Delafloxacin (MegluMine)
物理化學(xué)性質(zhì)
常見問題列表
德拉沙星葡甲胺(delafloxacin meglumine)由日本湧永制藥株式會社(Wakunaga Pharmaceutical Co. Ltd.)研制，1996年授予美國RIB-X制藥公司全球獨(dú)家開發(fā)權(quán)，由該公司旗下Melinta生物制藥公司全權(quán)負(fù)責(zé)研發(fā)、上市、生產(chǎn)和銷售。美國參議院為激勵抗菌藥物的研發(fā)，于2012年6月26日審議通過美國抗菌藥物研發(fā)法案，即《食品藥品管理局安全與創(chuàng)新法案》(FDASIA)。2014年尚處于Ⅲ期臨床試驗(yàn)的德拉沙星葡甲胺符合美國食品藥品管理局(FDA)制定的"合格的抗感染藥品"(QIDP)認(rèn)證條件，從而獲得優(yōu)先審評待遇，于2017年6月19日獲準(zhǔn)上市，商品名為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).
| 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. |