BAY179

BAY179 is a small molecule inhibitor of mitochondrial electron transport chain (ETC) Complex I, developed by Bayer. Unlike its predecessor BAY 87-2243, which is human-specific, BAY179 is designed to be cross-reactive between human and mouse Complex I, facilitating preclinical profiling in syngeneic and xenograft pharmacological models. Complex I inhibition disrupts the mitochondrial proton gradient and ATP synthesis, a pathway to which certain tumors—particularly those with LKB1 or mIDH mutations—exhibit heightened sensitivity. In preclinical studies, BAY179 demonstrated tumor growth inhibition in LKB1-deficient melanoma models, although its efficacy in vivo was limited by exposure constraints at the maximum tolerated dose (MTD) compared to human-specific analogs.