Bedaquiline

Bedaquiline is a diarylquinoline drug and inhibits Mycobacterium tuberculosis F1FO-ATP synthase by simultaneously targeting the subunit c and subunit ε. Bedaquiline has uncoupling activity and is used for the multi-drug resistant tuberculosis[1].

Bedaquiline has anticancer activity against cancer stem cell-like cells. Bedaquiline treatment of MCF7 breast cancer cells can inhibit mitochondrial oxygen consumption and glycolysis, but can induce oxidative stress. Bedaquiline can reduce mitochondrial membrane potential and significantly increase ROS levels[2].

Bedaquiline follows the principle of three-stage elimination, and its terminal half-life is very long, approximately 173 hours in humans[3].

References：

[1]. Jang J C, Jung Y G, Choi J, et al. Bedaquiline susceptibility test for totally drug-resistant tuberculosisMycobacterium tuberculosis. Journal of Microbiology, 2017, 55(6): 483-487.

[2]. Fiorillo M, Lamb R, Tanowitz H, et al. Bedaquiline, an FDA-approved antibiotic, inhibits mitochondrial function and potently blocks the proliferative expansion of stem-like cancer cells (CSCs). Aging, 2016, 8(8): 1593-1607.

[3]. Lakshmanan M, Xavier A S. Bedaquiline–The first ATP synthase inhibitor against multi drug resistant tuberculosis. Journal of Young Pharmacists, 2013, 5(4): 112-115.