Document Detail


The diarylquinoline TMC207 for multidrug-resistant tuberculosis.
MedLine Citation:
PMID:  19494215     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
BACKGROUND: The diarylquinoline TMC207 offers a new mechanism of antituberculosis action by inhibiting mycobacterial ATP synthase. TMC207 potently inhibits drug-sensitive and drug-resistant Mycobacterium tuberculosis in vitro and shows bactericidal activity in patients who have drug-susceptible pulmonary tuberculosis.
METHODS: In the first stage of a two-stage, phase 2, randomized, controlled trial, we randomly assigned 47 patients who had newly diagnosed multidrug-resistant pulmonary tuberculosis to receive either TMC207 (400 mg daily for 2 weeks, followed by 200 mg three times a week for 6 weeks) (23 patients) or placebo (24 patients) in combination with a standard five-drug, second-line antituberculosis regimen. The primary efficacy end point was the conversion of sputum cultures, in liquid broth, from positive to negative.
RESULTS: The addition of TMC207 to standard therapy for multidrug-resistant tuberculosis reduced the time to conversion to a negative sputum culture, as compared with placebo (hazard ratio, 11.8; 95% confidence interval, 2.3 to 61.3; P=0.003 by Cox regression analysis) and increased the proportion of patients with conversion of sputum culture (48% vs. 9%). The mean log(10) count of colony-forming units in the sputum declined more rapidly in the TMC207 group than in the placebo group. No significant differences in average plasma TMC207 concentrations were noted between patients with and those without culture conversion. Most adverse events were mild to moderate, and only nausea occurred significantly more frequently among patients in the TMC207 group than among patients in the placebo group (26% vs. 4%, P=0.04).
CONCLUSIONS: The clinical activity of TMC207 validates ATP synthase as a viable target for the treatment of tuberculosis. (ClinicalTrials.gov number, NCT00449644.)
Authors:
Andreas H Diacon; Alexander Pym; Martin Grobusch; Ramonde Patientia; Roxana Rustomjee; Liesl Page-Shipp; Christoffel Pistorius; Rene Krause; Mampedi Bogoshi; Gavin Churchyard; Amour Venter; Jenny Allen; Juan Carlos Palomino; Tine De Marez; Rolf P G van Heeswijk; Nacer Lounis; Paul Meyvisch; Johan Verbeeck; Wim Parys; Karel de Beule; Koen Andries; David F Mc Neeley
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Publication Detail:
Type:  Clinical Trial, Phase II; Journal Article; Multicenter Study; Randomized Controlled Trial    
Journal Detail:
Title:  The New England journal of medicine     Volume:  360     ISSN:  1533-4406     ISO Abbreviation:  N. Engl. J. Med.     Publication Date:  2009 Jun 
Date Detail:
Created Date:  2009-06-04     Completed Date:  2009-06-12     Revised Date:  2013-04-10    
Medline Journal Info:
Nlm Unique ID:  0255562     Medline TA:  N Engl J Med     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2397-405     Citation Subset:  AIM; IM    
Copyright Information:
2009 Massachusetts Medical Society
Affiliation:
Centre for Clinical Tuberculosis Research, the Department of Science and Technology, Faculty of Health Sciences, University of Stellenbosch, Tygerberg, all in South Africa.
Data Bank Information
Bank Name/Acc. No.:
ClinicalTrials.gov/NCT00449644
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MeSH Terms
Descriptor/Qualifier:
Adolescent
Adult
Antitubercular Agents / adverse effects,  pharmacokinetics,  therapeutic use*
Colony Count, Microbial
Drug Therapy, Combination
Female
Humans
Male
Microbial Sensitivity Tests
Middle Aged
Mycobacterium tuberculosis / drug effects*,  enzymology,  growth & development
Proton-Translocating ATPases / antagonists & inhibitors*
Quinolines / adverse effects,  pharmacokinetics,  therapeutic use*
Tuberculosis, Multidrug-Resistant / drug therapy*
Young Adult
Chemical
Reg. No./Substance:
0/Antitubercular Agents; 0/Quinolines; 78846I289Y/Bedaquiline; EC 3.6.3.14/Proton-Translocating ATPases
Comments/Corrections
Comment In:
N Engl J Med. 2009 Jun 4;360(23):2466-7   [PMID:  19494223 ]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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