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GSK2556286 Is a Novel Antitubercular Drug Candidate Effective <i>In Vivo</i> with the Potential To Shorten Tuberculosis Treatment

Eric L. Nuermberger, Maria Santos Martínez, Olalla Sanz, Beatriz Urones, Jorge Esquivias, Heena Soni, Rokeya Tasneen, Sandeep Tyagi, Si‐Yang Li, Paul J. Converse, Helena I. Boshoff, Gregory T. Robertson, Gurdyal S. Besra, Katherine A. Abrahams, Anna M. Upton, Khisimuzi Mdluli, Gary W. Boyle, Sam Turner, Nader Fotouhi, N. Cammack, Juan Miguel Siles, Marta Alonso, Jaime Escribano, Joël Lelièvre, Joaquin Rullas-Trincado, Esther Pérez‐Herrán, Robert H. Bates, Gareth Maher-Edwards, David Barros, Lluís Ballell, Elena Jiménez

2022Antimicrobial Agents and Chemotherapy48 citationsDOIOpen Access PDF

Abstract

] = 0.07 μM), is active against extracellular bacteria in cholesterol-containing culture medium, and exhibits no cross-resistance with known antitubercular drugs. In addition, it has shown efficacy in different mouse models of tuberculosis (TB) and has an adequate safety profile in two preclinical species. These features indicate a compound with a novel mode of action, although still not fully defined, that is effective against both multidrug-resistant (MDR) or extensively drug-resistant (XDR) and drug-sensitive (DS) M. tuberculosis with the potential to shorten the duration of treatment in novel combination drug regimens. (This study has been registered at ClinicalTrials.gov under identifier NCT04472897).

Topics & Concepts

Mycobacterium tuberculosisTuberculosisIn vivoDrugDrug resistanceMicrobiologyPharmacologyBacteriaMinimum inhibitory concentrationExtracellularMedicineAntibioticsBiologyVirologyBiotechnologyBiochemistryPathologyGeneticsTuberculosis Research and EpidemiologyEscherichia coli research studiesDrug Transport and Resistance Mechanisms
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