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Open AccessFeature PaperReview

Development of Delpazolid for the Treatment of Tuberculosis

by Young Lag Cho 1 and Jichan Jang 2,*
LegoChem Biosciences, Inc., 8-26 Munoyeongseo-ro, Daedeok-gu, Daejeon 34302, Korea
Molecular Mechanisms of Antibiotics, Division of Life Science, Research Institute of Life Sciences, Gyeongsang National University, Jinju 52828, Korea
Author to whom correspondence should be addressed.
Appl. Sci. 2020, 10(7), 2211;
Received: 3 March 2020 / Revised: 23 March 2020 / Accepted: 23 March 2020 / Published: 25 March 2020
(This article belongs to the Special Issue Tuberculosis Drug Discovery and Development 2019)
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. View Full-Text
Keywords: Mycobacterium tuberculosis; delpazolid; drug discovery; multi-drug resistance Mycobacterium tuberculosis; delpazolid; drug discovery; multi-drug resistance
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Cho, Y.L.; Jang, J. Development of Delpazolid for the Treatment of Tuberculosis. Appl. Sci. 2020, 10, 2211.

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