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Ganfeborole (GSK3036656) is a first-in-class investigational small molecule antitubercular agent developed for the treatment of tuberculosis. It acts as a selective inhibitor of the *Mycobacterium tuberculosis* enzyme leucyl-tRNA synthetase (LeuRS), thereby suppressing bacterial protein synthesis and exerting bactericidal activity against drug-susceptible, multidrug-resistant (MDR), and extensively drug-resistant (XDR) TB strains. The compound is an aminomethyl halogen benzoxaborole derivative that forms a covalent adduct with tRNA, blocking leucylation and halting protein synthesis in *M. tuberculosis*. Developed through collaboration between GSK and Anacor Pharmaceuticals, ganfeborole has demonstrated early bactericidal activity in Phase IIa clinical trials with good tolerability at low once-daily oral doses[1][2][3][4][5].
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