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