Bedaquiline is a member of the diarylquinoline class of drugs and has a unique mechanism of action, targeting the adenosine triphosphate (ATP) synthase enzyme of the TB mycobacteria. ATP-synthase is used in the process by which M.tb generates its energy supply. It is active against both M.tb and the drug-resistant TB bacteria that cause MDR-TB. Laboratory tests and clinical trials have shown it to have strong bactericidal and sterilizing properties.  

Developed by Janssen, In 2012, bedaquiline received conditional approved by the US FDA for the treatment of MDR-TB, in addition to the current second-line treatment regimen. A 2018 WHO Rapid Communication on MDR-TB treatment guidelines prioritized bedaquiline among the the drugs for treatment of MDR-TB. 

Bedaquiline is used in many of the new TB and drug-resistant TB treatment regimens currently in development by TB Alliance, as well as in the FDA-approved BPaL regimen.