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Overview
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Bedaquiline Fumarate (TMC-207) is a synthetic diarylquinoline made from equimolar amounts of Bedaquiline and Fumaric Acid. It acts as a proton-translocating ATP synthetase inhibitor. As an antimycobacterial and antitubercular agen, it inhibits the growth of Mycobacterium tuberculosis, the causal agent of tuberculosis. It was first described in 2004 by Janssen Phamaceuticals and is manufactured by Johnson &Johnson, and approved by the FDA in 2012, the first antitubercular agent in over 40 years.
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Background
Bedaquiline Fumarate has a unique mechanism of action as a proton-translocating mycobacterial ATP synthase inhibitor. It can bind to the oligomeric/proteolipid subunit c of the ATP synthase complex and prevent its function. The inhibitory effect of Bedaquiline on ATP synthase is specific for mycobacteria, as the ATP synthase complex in humans has 20,000 fold lower sensitivity to Bedaquiline compared with M. tuerculosis.
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Overview