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Bedaquiline (TMC207) is a diarylquinoline drug and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit[1]. Bedaquiline has uncoupler activity. Bedaquiline is used for the treatment of multi-drug resistant tuberculosis[2].

Bedaquiline inhibits the growth of TDR M. tuberculosis strains, with MIC values ranging from 0.125 to 0.5 mg/L[2]. Among slowly growing mycobacteria (SGM), bedaquiline exhibits the highest activity against Mycobacterium avium with MIC50 and MIC90 values of 0.03 and 16 mg/L, respectively. Among rapidly growing mycobacteria (RGM), Mycobacterium abscessus subsp. abscessus (M. abscessus) and Mycobacterium abscessus subsp. massiliense (M. massiliense) seem more susceptible to bedaquiline than Mycobacterium fortuitum, with MIC50 and MIC90 values of 0.13 and >16 mg/L, respectively, for both species. Bedaquiline also shows moderate in vitro activity against NTM species[3]. Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis[4].

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