Are moxifloxacin and levofloxacin equally effective to treat XDR tuberculosis?

Maitre, Thomas; Petitjean, G.; Chauffour, Aurélie; Bernard, Christine; Helali, Najoua El; Jarlier, Vincent; Reibel, Florence; Chavanet, P.; Aubry, Alexandra; Véziris, Nicolas

doi:10.1093/jac/dkx150

Cited by 27 publications

(29 citation statements)

References 37 publications

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“…Fluoroquinolones exhibit considerable anti-TB activities, although some of them such as ciprofloxacin, ofloxacin, and levofloacin are presently recommended as second-line anti-TB agents by WHO [6]; these drugs such as moxifloxacin (MXFX) are potential first-line agents and are under study for this indication [7]. In general, MTB isolates expressing resistance to both INH and RIF are susceptible to fluoroquinolones, while MXFX retains activity against MTB strains with various levels of fluoroquinolones resistance [8].…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and in vitro Anti‐mycobacterial Evaluation of Propylene‐1H‐1,2,3‐triazole‐4‐methylene‐tethered (Thio)semicarbazone‐isatin‐moxifloxacin Hybrids

Song

Fan

et al. 2017

Journal of Heterocyclic Chem

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A new class of propylene-1H-1,2,3-triazole-4-methylene-tethered (thio)semicarbazone-isatinmoxifloxacin hybrids 6a-h was designed, synthesized, and screened for their in vitro anti-mycobacterial activities against Mycobacterium tuberculosis (MTB) H 37 Rv and MDR-TB as well as cytotoxicity in VERO cell line. All the synthesized hybrids (MIC: 0.05-2.0 μg/mL) exhibited excellent activities against M. tuberculosis H 37 Rv and MDR-TB; in particular, conjugate 6c (MIC: 0.05 and 0.12 μg/mL) was no inferior to the three references MXFX (MIC: 0.10 and 0.12 μg/mL), RIF (MIC: 0.39 and 32 μg/mL), and INH (MIC: 0.05 and >128 μg/mL) against the tested two strains. All hybrids (CC 50 : 2-8 μg/mL) were much more cytotoxic than the parent MXFX (CC 50 : 128 μg/mL) should be further optimized.

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Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and in vitro Anti‐mycobacterial Evaluation of Propylene‐1H‐1,2,3‐triazole‐4‐methylene‐tethered (Thio)semicarbazone‐isatin‐moxifloxacin Hybrids

Song

Fan

et al. 2017

Journal of Heterocyclic Chem

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“…The pre-XDR and XDR-TB patients in this study were managed with regimens which contained levofloxacin. Previous studies have shown that in cases of levofloxacin resistance, moxifloxacin may be the preferred drug of choice since gyrA A90V mutation has a smaller effect on moxifloxacin activity [8,26]. Therefore, these patients could have benefited from a regimen containing Moxifloxacin if the specific resistance markers had been determined timely.…”

Section: Discussionmentioning

confidence: 99%

Detection of Second Line Drug Resistance among Drug Resistant Mycobacterium Tuberculosis Isolates in Botswana

et al. 2019

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The emergence and transmission of multidrug resistant (MDR) and extensively drug resistant (XDR) Mycobacterium tuberculosis (M.tb) strains is a threat to global tuberculosis (TB) control. The early detection of drug resistance is critical for patient management. The aim of this study was to determine the proportion of isolates with additional second-line resistance among rifampicin and isoniazid resistant and MDR-TB isolates. A total of 66 M.tb isolates received at the National Tuberculosis Reference Laboratory between March 2012 and October 2013 with resistance to isoniazid, rifampicin or both were analyzed in this study. The genotypes of the M.tb isolates were determined by spoligotyping and second-line drug susceptibility testing was done using the Hain Genotype MTBDRsl line probe assay version 2.0. The treatment outcomes were defined according to the Botswana national and World Health Organization (WHO) guidelines. Of the 57 isolates analyzed, 33 (58%) were MDR-TB, 4 (7%) were additionally resistant to flouroquinolones and 3 (5%) were resistant to both fluoroquinolones and second-line injectable drugs. The most common fluoroquinolone resistance-conferring mutation detected was gyrA A90V. All XDR-TB cases remained smear or culture positive throughout the treatment. Our study findings indicate the importance of monitoring drug resistant TB cases to ensure rapid detection of second-line drug resistance.

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“…In addition, quinolones especially fluoroquinolones were widely used as antibiotics, and WHO has recommended some of fluoroquinolones including ciprofloxacin, ofloxacin, and levofloxacin as second‐line anti‐TB agents for the treatment of patients with resistance or intolerance to first‐line anti‐TB therapy . Furthermore, the fourth generation fluoroquinolone moxifloxacin is under phase III clinical trial as a potential first‐line anti‐TB agent . Therefore, hybridization of quinoline with isatin appears to be an attractive strategy to develop high effective anti‐TB agents.…”

Section: Isatin‐quinoline/quinolone Hybridsmentioning

confidence: 99%

Isatin Derivatives with Potential Antitubercular Activities

Jiang

Wang

Liu

et al. 2018

Journal of Heterocyclic Chem

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Tuberculosis is a life‐threatening chronic infectious disease, which primarily affects the lungs but can spread to other vital organs. The re‐emergence and wide spread of new virulent forms of Mycobacterium tuberculosis that are resistant to some or all first and second line antitubercular agents has reached an alarming level in recent decades. Thus, it is imperative to develop more effective agents. Isatin derivatives are endowed with diverse biological properties, therefore thousands of isatin derivatives have been synthesized in hopes of discovering new candidates with potential antitubercular activities against both drug‐susceptible and drug‐resistant strains. This review summarizes the recent developments of isatin derivatives with potential antitubercular activities.

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Are moxifloxacin and levofloxacin equally effective to treat XDR tuberculosis?

Abstract: All mutations reduced fluoroquinolone activity, even those classified as susceptible according to phenotypic tests. High-dose levofloxacin is less effective than high-dose moxifloxacin against both fluoroquinolone-resistant and -susceptible M. tuberculosis strains in mice.

Cited by 27 publications

References 37 publications

Design, Synthesis, and in vitro Anti‐mycobacterial Evaluation of Propylene‐1H‐1,2,3‐triazole‐4‐methylene‐tethered (Thio)semicarbazone‐isatin‐moxifloxacin Hybrids

Design, Synthesis, and in vitro Anti‐mycobacterial Evaluation of Propylene‐1H‐1,2,3‐triazole‐4‐methylene‐tethered (Thio)semicarbazone‐isatin‐moxifloxacin Hybrids

Detection of Second Line Drug Resistance among Drug Resistant Mycobacterium Tuberculosis Isolates in Botswana

Isatin Derivatives with Potential Antitubercular Activities

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