{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,25]],"date-time":"2026-09-25T15:51:34Z","timestamp":1790351494095,"version":"4.1.0"},"reference-count":42,"publisher":"SAGE Publications","issue":"1","license":[{"start":{"date-parts":[[2013,11,1]],"date-time":"2013-11-01T00:00:00Z","timestamp":1383264000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.sagepub.com\/page\/policies\/text-and-data-mining-license"}],"content-domain":{"domain":["journals.sagepub.com"],"crossmark-restriction":true},"short-container-title":["Ann Pharmacother"],"published-print":{"date-parts":[[2014,1]]},"abstract":"<jats:p>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.<\/jats:p>","DOI":"10.1177\/1060028013504087","type":"journal-article","created":{"date-parts":[[2014,1,21]],"date-time":"2014-01-21T15:04:57Z","timestamp":1390316697000},"page":"107-115","update-policy":"https:\/\/doi.org\/10.1177\/sage-journals-update-policy","source":"Crossref","is-referenced-by-count":107,"title":["Bedaquiline"],"prefix":"10.1177","volume":"48","author":[{"given":"Elias B.","family":"Chahine","sequence":"first","affiliation":[{"name":"Palm Beach Atlantic University, West Palm Beach, FL, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lamis R.","family":"Karaoui","sequence":"additional","affiliation":[{"name":"Lebanese American University, Byblos, Lebanon"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hanine","family":"Mansour","sequence":"additional","affiliation":[{"name":"Lebanese American University, Byblos, Lebanon"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"179","published-online":{"date-parts":[[2013,11,1]]},"reference":[{"key":"bibr1-1060028013504087","unstructured":"World Health Organization. Tuberculosis fact sheets. http:\/\/www.who.int\/mediacentre\/factsheets\/fs104\/en\/. Accessed May 7, 2012."},{"key":"bibr2-1060028013504087","unstructured":"World Health Organization. Multidrug-resistant tuberculosis (MDR-TB): 2012 update. http:\/\/www.who.int\/tb\/publications\/MDRFactSheet2012.pdf. Accessed May 7, 2013."},{"key":"bibr3-1060028013504087","doi-asserted-by":"publisher","DOI":"10.5455\/2319-2003.ijbcp20130301"},{"key":"bibr4-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1183\/09031936.00168008"},{"key":"bibr5-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1183\/09031936.00204611"},{"key":"bibr6-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1183\/09031936.00027612"},{"key":"bibr7-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1086\/653115"},{"key":"bibr8-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1016\/S0140-6736(06)69573-1"},{"key":"bibr9-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1038\/nbt0205-187"},{"key":"bibr10-1060028013504087","unstructured":"Sirturo (bedaquiline) [product information]. Titusville, NJ: Janssen Therapeutics; 2012."},{"key":"bibr11-1060028013504087","doi-asserted-by":"publisher","DOI":"10.2217\/fmb.10.50"},{"key":"bibr12-1060028013504087","doi-asserted-by":"publisher","DOI":"10.2174\/157340607780620626"},{"key":"bibr13-1060028013504087","unstructured":"FDA news release [untitled]. http:\/\/www.fda.gov\/NewsEvents\/Newsroom\/PressAnnouncements\/ucm333695.htm. Accessed May 7, 2013."},{"key":"bibr14-1060028013504087","unstructured":"Bedaquiline clinical trials. http:\/\/www.clinicaltrials.gov\/ct2\/results?term=bedaquiline. Accessed May 7, 2013."},{"key":"bibr15-1060028013504087","first-page":"1561","volume-title":"Goodman and Gilman\u2019s The Pharmacological Basis of Therapeutics","author":"Gumbo T","year":"2011","edition":"12"},{"key":"bibr16-1060028013504087","unstructured":"Bedaquiline: compound summary. http:\/\/pubchem.ncbi.nlm.nih.gov\/summary\/summary.cgi?cid=5388906&loc=ec_rcs. Accessed May 22, 2013."},{"key":"bibr17-1060028013504087","unstructured":"Bedaquiline fumarate: compound summary. http:\/\/pubchem.ncbi.nlm.nih.gov\/summary\/summary.cgi?cid=56841861. Accessed May 18, 2013."},{"key":"bibr18-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1126\/science.1106753"},{"key":"bibr19-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00181-07"},{"key":"bibr20-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.50.4.1558-1560.2006"},{"key":"bibr21-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00244-06"},{"key":"bibr22-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1126\/science.1108379"},{"key":"bibr23-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1056\/NEJMoa0808427"},{"key":"bibr24-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00720-11"},{"key":"bibr25-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1586\/eri.10.60"},{"key":"bibr26-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.06126-11"},{"key":"bibr27-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.02243-12"},{"key":"bibr28-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.01204-07"},{"key":"bibr29-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00766-06"},{"key":"bibr30-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1016\/j.tube.2010.07.004"},{"key":"bibr31-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1164\/rccm.200807-1152OC"},{"key":"bibr32-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00898-06"},{"key":"bibr33-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1016\/S0140-6736(12)61080-0"},{"key":"bibr34-1060028013504087","unstructured":"McNeely DF, Diacon AH, Pym A, TMC-207 versus placebo plus OBT for the treatment of MDR-TB: a prospective clinical trial. Oral Presentation at: 41st Union World Conference on Lung Health; November 13, 2010; Berlin, Germany. http:\/\/uwclh.conference2web.com\/content\/187?from_view=all&view_address=search%3Dmcneeley%26events%3D1%26groups%3D1%26sessions%3D35. Accessed May 30, 2013."},{"key":"bibr35-1060028013504087","unstructured":"Haxaire M, TMC207 Team, Diacon AH, Use of bedaquiline (TMC207) for the treatment of MDR-TB. Data presented at: 43rd Union World Conference on Lung Health; November 16, 2012; Kuala Lumpur, Malaysia. http:\/\/uwclh.conference2web.com\/content\/2168\/details?from_view=all&view_address=search%3Dhaxaire%26events%3D3%26sessions%3D301. Accessed May 30, 2013."},{"key":"bibr36-1060028013504087","unstructured":"Haxaire M, TMC207 Team, Diacon AH, Phase 2 open-label trial of TMC207 in an MDR-TB treatment regimen. Data presented at: 42nd Union World Conference on Lung Health; October 30, 2011; Lille, France. http:\/\/uwclh.conference2web.com\/content\/1108\/details?from_view=all&view_address=search%3Dhaxaire%26events%3D2. Accessed May 30, 2013."},{"key":"bibr37-1060028013504087","unstructured":"Anti-Infective Drugs Advisory Committee Meeting Briefing Document TMC207 (bedaquiline) Treatment of Patients with MDR-TB. http:\/\/www.fda.gov\/downloads\/AdvisoryCommittees\/CommitteesMeetingMaterials\/Drugs\/Anti-InfectiveDrugsAdvisoryCommittee\/UCM329260.pdf. Accessed May 31, 2013."},{"key":"bibr38-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1097\/QAI.0b013e3182410503"},{"key":"bibr39-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.00191-13"},{"key":"bibr40-1060028013504087","unstructured":"Centers for Disease Control and Prevention. Reported Tuberculosis in the United States, 2011. Atlanta, GA: US Department of Health and Human Services, Centers for Disease Control and Prevention; 2012. http:\/\/www.cdc.gov\/tb\/statistics\/reports\/2011. Accessed May 7, 2013."},{"key":"bibr41-1060028013504087","doi-asserted-by":"publisher","DOI":"10.1126\/science.339.6116.130"},{"key":"bibr42-1060028013504087","unstructured":"Red Book Online. http:\/\/www.redbook.com\/redbook\/online. Accessed September 13, 2013."}],"container-title":["Annals of Pharmacotherapy"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/journals.sagepub.com\/doi\/pdf\/10.1177\/1060028013504087","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/journals.sagepub.com\/doi\/full-xml\/10.1177\/1060028013504087","content-type":"application\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/journals.sagepub.com\/doi\/pdf\/10.1177\/1060028013504087","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2026,4,28]],"date-time":"2026-04-28T11:14:26Z","timestamp":1777374866000},"score":1,"resource":{"primary":{"URL":"https:\/\/journals.sagepub.com\/doi\/10.1177\/1060028013504087"}},"subtitle":["A Novel Diarylquinoline for Multidrug-Resistant Tuberculosis"],"short-title":[],"issued":{"date-parts":[[2013,11,1]]},"references-count":42,"journal-issue":{"issue":"1","published-print":{"date-parts":[[2014,1]]}},"alternative-id":["10.1177\/1060028013504087"],"URL":"https:\/\/doi.org\/10.1177\/1060028013504087","relation":{},"ISSN":["1060-0280","1542-6270"],"issn-type":[{"value":"1060-0280","type":"print"},{"value":"1542-6270","type":"electronic"}],"subject":[],"published":{"date-parts":[[2013,11,1]]}}}