Biochem/physiol Actions
Potent and selective mycobacterial ATP synthase inhibitor with broad-spectrum anti-mycobacterial activity.
TMC207 (Bedaquiline; R207910) is an orally active, potent and selective mycobacterial ATP synthase inhibitor (M. smegmatis IC50 = 2.5 nM or 1.4 ng (non-salt form)/mL; human mitochondrial ATP syntase IC50 >200 uM) with broad-spectrum anti-mycobacterial activity (MIC 10-120 ng/mL), including M. bovis, avium complex (MAC), kansasii, marinum, fortuitum, abscessus, smegmatis, ulcerans, and both drug-susceptible and multiple drug-resistant M. tuberculosis strains (to rigampin, isoniazid, streptomycin, ethambutol, pyrazinamide, fluoroquinolone).