In vivo pharmacodynamic study of contezolid acefosamil, a prodrug of contezolid for oral and intravenous administration

Author:

Wang Xiu-Kun1,Yu Jie1,Xie Chun-Yang1,Hu Xin-Xin1,Nie Tong-Ying1,Li Xue1,Wang Peng-He1,Li Guo-Qing1,Yuan Hong2,Yang Xin-Yi1,Li Cong-Ran1,You Xue-Fu1ORCID

Affiliation:

1. Beijing Key laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College , Beijing , China

2. Shanghai MicuRx Pharmaceutical Co., Ltd , Shanghai , China

Abstract

Abstract 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.

Funder

National Natural Science Foundation of China

CAMS

Publisher

Oxford University Press (OUP)

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology,Microbiology (medical)

Reference17 articles.

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