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Review
. 2014 Jan;48(1):107-15.
doi: 10.1177/1060028013504087. Epub 2013 Nov 1.

Bedaquiline: a novel diarylquinoline for multidrug-resistant tuberculosis

Affiliations
Review

Bedaquiline: a novel diarylquinoline for multidrug-resistant tuberculosis

Elias B Chahine et al. Ann Pharmacother. 2014 Jan.

Abstract

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.

Keywords: MDR-TB; antimycobacterial; bedaquiline; diarylquinoline; multi-drug resistant tuberculosis.

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Comment in

  • Current issues with the use of bedaquiline.
    Kakkar AK, Dahiya N. Kakkar AK, et al. Ann Pharmacother. 2014 May;48(5):666. doi: 10.1177/1060028014521589. Epub 2014 Feb 11. Ann Pharmacother. 2014. PMID: 24519480 No abstract available.
  • Reply to comments by Kakkar and Dahiya.
    Chahine EB, Karaoui L, Mansour H. Chahine EB, et al. Ann Pharmacother. 2014 May;48(5):667. doi: 10.1177/1060028014521590. Ann Pharmacother. 2014. PMID: 24733170 No abstract available.

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