Development of Delpazolid for the Treatment of Tuberculosis

Abstract

A novel oxazolidinone with cyclic amidrazone, delpazolid (LCB01-0371), was synthesized by LegoChem BioSciences, Inc. (Daejeon, Korea). Delpazolid can improve the minimum bactericidal concentration of Mycobacterium tuberculosis H37Rv and significantly reduce resistance rates, especially of multi-drug-resistant tuberculosis (MDR-TB) isolates, compared with linezolid. Therefore, delpazolid can be used to treat MDR-TB. The safety, tolerability, and pharmacokinetics of delpazolid have been evaluated in a phase 1 clinical trial, which revealed that it does not cause adverse events such as myelosuppression even after three weeks of repeated dosing. Interim efficacy and safety results, particularly those from a clinical phase 2a early bactericidal activity trial including patients with drug-susceptible tuberculosis, were reported and the findings will be further analyzed to guide phase 2a studies.

Keywords

• <i>mycobacterium tuberculosis</i>
• delpazolid
• drug discovery
• multi-drug resistance