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Open AccessFeature PaperReview

Development of Delpazolid for the Treatment of Tuberculosis

by Young Lag Cho 1 and Jichan Jang 2,*
1
LegoChem Biosciences, Inc., 8-26 Munoyeongseo-ro, Daedeok-gu, Daejeon 34302, Korea
2
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; https://doi.org/10.3390/app10072211
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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