AR-C155858

AR-C155858 is a potent and selective small molecule inhibitor of monocarboxylate transporters 1 and 2 (MCT1 and MCT2). Developed by AstraZeneca, it functions by blocking the transmembrane transport of lactate, which is a critical metabolic byproduct in glycolytic cancer cells. Inhibition of MCT1/2 leads to the accumulation of intracellular lactate, resulting in decreased intracellular pH and the inhibition of glycolysis and cell proliferation. In preclinical studies, AR-C155858 has demonstrated efficacy in reducing tumor growth and re-sensitizing resistant cancer cells, such as enzalutamide-resistant prostate cancer, to standard therapies. Although primarily utilized as a pharmacological tool in research, its profile supported the advancement of related compounds into clinical trials.