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WQ-3810: A new fluoroquinolone with a high potential against fluoroquinolone-resistant Mycobacterium tuberculosis

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Title: WQ-3810: A new fluoroquinolone with a high potential against fluoroquinolone-resistant Mycobacterium tuberculosis
Authors: Ouchi, Yuki Browse this author
Mukai, Tetsu Browse this author
Koide, Kentaro Browse this author
Yamaguchi, Tomoyuki Browse this author
Park, Jong-Hoon Browse this author
Kim, Hyun Browse this author
Yokoyama, Kazumasa Browse this author
Tamaru, Aki Browse this author
Gordon, Stephen V. Browse this author
Nakajima, Chie Browse this author →KAKEN DB
Suzuki, Yasuhiko Browse this author →KAKEN DB
Keywords: WQ-3810
Fluoroquinolone resistance
gyrA mutations
Mycobacterium tuberculosis
Synergistic effect
Issue Date: Jan-2020
Publisher: Elsevier
Journal Title: Tuberculosis
Volume: 120
Start Page: 101891
Publisher DOI: 10.1016/
Abstract: Fluoroquinolone (FQ) resistance in Mycobacterium tuberculosis (Mtb), caused by amino acid substitutions in DNA gyrase, has been increasingly reported worldwide. WQ-3810 is a newly developed FQ that is highly active against FQ-resistant pathogens; however, its activity against Mtb has not been evaluated. Herein we examined the efficacy of WQ-3810 against Mtb through the use of recombinant Mtb DNA gyrases. In addition, in vitro anti-mycobacterial activity of WQ-3810 was evaluated against recombinant Mtb var. bovis Bacille Calmette-Guerin strains in which gyrase-coding genes were replaced with Mtb variants containing resistance-conferring mutations. WQ-3810 showed a higher inhibitory activity than levofloxacin against most recombinant DNA gyrases with FQ-resistance mutations. Furthermore, WQ-3810 showed inhibition even against a DNA gyrase variant harboring a G88C mutation which is thought to confer the highest resistance against FQs in clinical Mtb isolates. In contrast, the FQ susceptibility test showed that WQ-3810 had relatively weak mycobactericidal activity compared with moxifloxacin. However, the combination of WQ-3810 and ethambutol showed the greatest degree of synergistic activity against recombinant strains. Since FQs and ethambutol have been used in multi-drug therapy for tuberculosis, WQ-3810 might represent a new, potent anti-tuberculosis drug that can be effective even against FQ-resistant Mtb strains.
Rights: ©2020. This manuscript version is made available under the CC-BY-NC-ND 4.0 license
Type: article (author version)
Appears in Collections:人獣共通感染症国際共同研究所 (International Institute for Zoonosis Control) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 鈴木 定彦

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