Antimicrobial Agents and Chemotherapy · 2013 · 183 citations · 15 references
MedicinePharmacologyPharmacotherapyAntimicrobial PharmacologyAntimicrobial PharmacotherapyChemotherapyAntibacterial ResistanceAntimicrobial PharmacodynamicsCellular Drug EffluxEfflux-mediated ResistanceEnzyme InhibitionTuberculosis PharmacotherapyChemotherapeutic EffluxDrug Efflux MechanismsEfflux Transporter InhibitionMolecular Drug ResistanceMycobacterium Tuberculosis InfectionResistance In Clinical IsolatesTuberculosis Drug ResistanceVerapamil Therapy
Drug efflux is an important resistance mechanism in Mycobacterium tuberculosis. We found that verapamil, an efflux inhibitor, profoundly decreases the MIC of bedaquiline and clofazimine to M. tuberculosis by 8- to 16-fold. This exquisite susceptibility was noted among drug-susceptible and drug-resistant clinical isolates. Thus, efflux inhibition is an important sensitizer of bedaquiline and clofazimine, and efflux may emerge as a resistance mechanism to these drugs.
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A Diarylquinoline Drug Active on the ATP Synthase of <i>Mycobacterium tuberculosis</i>
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