Development of Delpazolid for the Treatment of Tuberculosis
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 <i>Mycobacterium tuberculosis </i>H37Rv and significantly reduce resistance rates, espec...
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doaj-9d0416edba744667960cca5eb07992e82020-11-25T01:44:35ZengMDPI AGApplied Sciences2076-34172020-03-01107221110.3390/app10072211app10072211Development of Delpazolid for the Treatment of TuberculosisYoung Lag Cho0Jichan Jang1LegoChem Biosciences, Inc., 8-26 Munoyeongseo-ro, Daedeok-gu, Daejeon 34302, KoreaMolecular Mechanisms of Antibiotics, Division of Life Science, Research Institute of Life Sciences, Gyeongsang National University, Jinju 52828, KoreaA novel oxazolidinone with cyclic amidrazone, delpazolid (LCB01-0371), was synthesized by LegoChem BioSciences, Inc. (Daejeon, Korea). Delpazolid can improve the minimum bactericidal concentration of <i>Mycobacterium tuberculosis </i>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.https://www.mdpi.com/2076-3417/10/7/2211<i>mycobacterium tuberculosis</i>delpazoliddrug discoverymulti-drug resistance |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Young Lag Cho Jichan Jang |
spellingShingle |
Young Lag Cho Jichan Jang Development of Delpazolid for the Treatment of Tuberculosis Applied Sciences <i>mycobacterium tuberculosis</i> delpazolid drug discovery multi-drug resistance |
author_facet |
Young Lag Cho Jichan Jang |
author_sort |
Young Lag Cho |
title |
Development of Delpazolid for the Treatment of Tuberculosis |
title_short |
Development of Delpazolid for the Treatment of Tuberculosis |
title_full |
Development of Delpazolid for the Treatment of Tuberculosis |
title_fullStr |
Development of Delpazolid for the Treatment of Tuberculosis |
title_full_unstemmed |
Development of Delpazolid for the Treatment of Tuberculosis |
title_sort |
development of delpazolid for the treatment of tuberculosis |
publisher |
MDPI AG |
series |
Applied Sciences |
issn |
2076-3417 |
publishDate |
2020-03-01 |
description |
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 <i>Mycobacterium tuberculosis </i>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. |
topic |
<i>mycobacterium tuberculosis</i> delpazolid drug discovery multi-drug resistance |
url |
https://www.mdpi.com/2076-3417/10/7/2211 |
work_keys_str_mv |
AT younglagcho developmentofdelpazolidforthetreatmentoftuberculosis AT jichanjang developmentofdelpazolidforthetreatmentoftuberculosis |
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