OBJECTIVE: To review the chemistry, pharmacology, microbiology, 
pharmacokinetics, pharmacodynamics, clinical efficacy, safety, dosage, and 
administration of bedaquiline, a novel oral diarylquinoline antimycobacterial 
agent approved by the Food and Drug Administration for the treatment of adults 
with pulmonary multidrug-resistant tuberculosis (MDR-TB).
DATA SOURCES: A search of PubMed (January 2004-May 2013) and International 
Pharmaceutical Abstracts (January 2004-May 2013) using the search terms 
bedaquiline, diarylquinoline, R207910, and TMC207 was performed. Supplementary 
sources included proceedings of the Union World Conference on Lung Health.
STUDY SELECTION AND DATA EXTRACTION: Preclinical data as well as Phase 1 and 2 
studies published in English were evaluated.
DATA SYNTHESIS: Bedaquiline possesses a unique mechanism of action that disrupts 
the activity of the mycobacterial adenosine triphosphate synthase. Clinical 
trials have been conducted evaluating the use of bedaquiline in combination with 
a background regimen for the treatment of adults with pulmonary MDR-TB. 
Bedaquiline has an excellent in vitro activity against Mycobacterium 
tuberculosis, including multidrug resistant M tuberculosis; however, its side 
effect profile limits its use against MDR-TB when no other effective regimen can 
be provided. Bedaquiline carries Black Box warnings for increased risk of 
unexplained mortality and QT prolongation. Bedaquiline is metabolized via the 
CYP3A4 isoenzyme and thus interacts with rifamycins and several antiretrovirals.
CONCLUSIONS: In an era of emerging resistance and given the suboptimal efficacy 
and toxicity of currently available regimens for MDR-TB, bedaquiline represents 
a great addition to the existing armamentarium of anti-TB agents particularly in 
areas of the world where the disease is endemic.