With the strategy of repurposing FDA-approved drugs for the therapy of diabetes, we performed a high-throughput MST1 inhibition screen across a highly privileged collection of 641 drug-like kinase inhibitors, together with a triaging strategy for selective, non-cytotoxic compounds, and identified neratinib, approved for breast cancer and in clinical studies for lung, colorectal, and bladder cancers targeting human epidermal growth factor receptor 2 (EGFR2, also named HER2 and ErbB2) and EGFR dual kinases, as potent MST1 inhibitor3. The gene discussed is ERBB2; the disease is urinary bladder cancer.