康替唑胺氨丁三醇体内药效学研究：康替唑胺的前药，用于口服和静脉给药。
In vivo pharmacodynamic study of contezolid acefosamil, a prodrug of contezolid for oral and intravenous administration.
机构信息
Beijing Key laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, China.
Shanghai MicuRx Pharmaceutical Co., Ltd, Shanghai, China.
出版信息
J Antimicrob Chemother. 2023 Jul 5;78(7):1632-1636. doi: 10.1093/jac/dkad138.
OBJECTIVES
Contezolid acefosamil is a novel O-acyl phosphoramidate prodrug of contezolid. In the current study, we aimed to systemically evaluate the efficacy of contezolid acefosamil against infections caused by multiple Gram-positive pathogens, and compare the efficacy of the prodrug by oral and intravenous administrations.
METHODS
The in vivo pharmacodynamic efficacy of contezolid acefosamil was evaluated in mouse models of systemic (with five S. aureus, three S. pneumoniae and two S. pyogenes bacterial isolates) and thigh (with two S. aureus isolates) infections using linezolid as the reference agent.
RESULTS
In both models, contezolid acefosamil administrated either orally or intravenously, demonstrated high antibacterial efficacy similar to linezolid, and the antibacterial efficacy of oral and intravenous contezolid acefosamil were comparable.
CONCLUSIONS
The high aqueous solubility and great efficacy of contezolid acefosamil support its clinical development as an injectable and oral antibiotic suitable for serious Gram-positive infections.
目的
康替唑肟磷酰氨酯是康替唑的新型 O-酰基磷酰胺酯前药。在本研究中，我们旨在系统评估康替唑肟磷酰氨酯治疗多种革兰氏阳性病原体感染的疗效，并比较口服和静脉给药两种制剂的疗效。
方法
采用利奈唑胺作为参比药物，在全身性（5 株金黄色葡萄球菌、3 株肺炎链球菌和 2 株化脓性链球菌分离株）和大腿（2 株金黄色葡萄球菌分离株）感染的小鼠模型中评估康替唑肟磷酰氨酯的体内药效学疗效。
结果
在两种模型中，口服或静脉注射康替唑肟磷酰氨酯均表现出与利奈唑胺相似的高抗菌疗效，且口服和静脉注射康替唑肟磷酰氨酯的抗菌疗效相当。
结论
康替唑肟磷酰氨酯具有高水溶性和优异的疗效，支持其作为一种适合严重革兰氏阳性感染的可注射和口服抗生素进行临床开发。
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