Description
Bedaquiline is a diarylquinoline found to be useful in treating multidrug-resistant tuberculosis. In mouse models of TB, bedaquiline has significantly shortened the treatment regimen. A long-acting injectable formulation has been shown to have prolonged bactericidal activity.
Bedaquiline inhibits ATP-synthase, and at high concentrations leads to suppression of oxidative phosphorylation. In rat liver mitochondria, bedaquiline suppresses the formation of MPT pores, which typically accompanies the development of tuberculosis. Several analogues of bedaquiline that may improve its bioavailability are also in development.