Concentration of contezolid in cerebrospinal fluid and serum in a patient with tuberculous meningoencephalitis: A case report.

Abstract

Central nervous system (CNS) tuberculosis (TB) is a devastating and often life-threatening disease caused by Mycobacterium tuberculosis. Contezolid, a new oxazolidinone, has demonstrated potent antimycobacterial activity in both in-vivo and in-vitro studies, with lower toxicity than linezolid. However, pharmacokinetic data are still not available for contezolid in the CNS of patients with CNS TB. This article reports the steady-state concentrations of contezolid in serum and cerebrospinal fluid (CSF) of a patient receiving contezolid as part of multi-drug treatment for tuberculous meningoencephalitis. At weeks 7 and 11 (7 h post-dose) after initiation of contezolid therapy, the serum concentrations of contezolid were 9.64 mg/L and 9.36 mg/L, respectively. In CSF, the observed concentrations of contezolid were 0.54 mg/L and 1.15 mg/L, respectively. The CSF:serum concentration ratios were 0.056 and 0.123 at weeks 7 and 11, respectively. The observed concentrations in CSF were above the minimum inhibitory concentration of contezolid against M. tuberculosis, and were close to the estimated serum unbound fraction of contezolid (10%), suggesting that unbound contezolid has high CSF permeability.

• Authors: Wanru Guo, Ming Hu, Nana Xu, Yanwan Shangguan, Jiafeng Xia, Wenjuan Hu, Xiaomeng Li, Qingwei Zhao, Kaijin Xu
• Journal: International journal of antimicrobial agents (Int J Antimicrob Agents) Vol. 62 Issue 2 Pg. 106875 (Aug 2023) ISSN: 1872-7913 [Electronic] Netherlands
• PMID: 37276894 (Publication Type: Case Reports, Journal Article)
• Copyright: Copyright © 2023 The Author(s). Published by Elsevier Ltd.. All rights reserved.

Chemical References

• contezolid
• Oxazolidinones
• Pyridones

Topics

• Humans
• Oxazolidinones
• Tuberculosis, Meningeal (drug therapy)
• Pyridones
• Mycobacterium tuberculosis
• Meningoencephalitis (drug therapy)
• Cerebrospinal Fluid