Bedaquiline is a diarylquinoline antitubercular drug with a novel mechanism of 
action against Mycobacterium tuberculosis. Bedaquiline works by inhibiting 
bacterial adenosine triphosphate (ATP) synthase and represents the first novel 
class of antituberculosis agents in more than 40 years. Bedaquiline is indicated 
for the treatment of multidrug-resistant tuberculosis (MDR TB) in combination 
with at least three other antitubercular drugs when no other effective regimen 
is available. The recommended bedaquiline dosage is 400 mg orally once/day for 2 
weeks followed by 200 mg orally 3 times/week for 22 weeks. Bedaquiline should be 
administered with food, which increases the bioavailability 2-fold. Bedaquiline 
is metabolized by cytochrome P450 isoenzyme 3A4 and is impacted by both inducers 
and inhibitors of this isoenzyme. Concentration-dependent bactericidal activity 
was observed in laboratory and murine studies. Accelerated approval was granted 
in the United States and European Union based on the results of two phase IIb 
clinical studies that used sputum culture clearance as a surrogate end point for 
clinical efficacy. These studies showed greater sputum culture clearance up to 
week 24 for the bedaquiline group compared with placebo. Common adverse events 
in clinical trials included nausea, arthralgia, and headache. Serious adverse 
events included elevated serum transaminase levels and rate-corrected 
QT-interval prolongation. Unexplained higher mortality was seen in patients 
receiving bedaquiline versus those receiving placebo. Bedaquiline is a novel 
agent with a unique mechanism of action and has the potential to meet a great 
need in patients with MDR TB who have no other treatment options. Due to safety 
concerns and limited clinical information, phase III trials are needed to fully 
determine its place in therapy.