TMC207 (Bedaquiline) is a diarylquinoline-based inhibitor of bacterial ATP synthase at nanomolar concentrations. In vitro mycobacterial experiments show that TMC207 inhibits drug-sensitive and drug-resistant mycobacterial TB at an MIC range of 2 to 60 nM and an MIC50 of 30 ng/mL. Additionally TMC207 is broadly potent against many non-tuberculous mycobacteria, with MICs of 6 to 500 nM. (1)

Studies show that TMC207 is orally-available and efficacious on a once-daily administration for patients with pulmonary TB. No serious adverse events were observed. (2)