Researchers from National Health Research Institutes reported the discovery and preclinical characterization of a novel long half-life Aurora A (AURKA) inhibitor being developed for the treatment of MYC-amplified solid tumors. Lead optimization of a previously reported series of small-molecule Aurora kinase inhibitors led to the discovery of AURKA kinase inhibitor 6K465, which was then developed into the acyl-based prodrug DBPR-728.