TBAJ-587

TBAJ-587 is a novel small molecule diarylquinoline developed as an anti-tuberculosis agent. It acts by directly inhibiting the F-ATP synthase c subunit in mycobacteria, disrupting the electron transport chain and energy production within Mycobacterium tuberculosis and nontuberculous mycobacteria (NTM) such as Mycobacterium abscessus. Compared to bedaquiline, TBAJ-587 demonstrates higher anti-tuberculosis activity, lower lipophilicity, weaker inhibition of hERG channels (suggesting a potentially improved cardiac safety profile), and superior efficacy in preclinical models. It exhibits potent bactericidal activity both extracellularly and intracellularly against M. abscessus, with comparable or better performance than bedaquiline in animal models. The drug is being evaluated for its potential to be part of new oral regimens for multidrug-resistant tuberculosis (MDR-TB) and NTM infections[1][2][4][5].