As a complement and update of previously reviewed articles detailing the clinical relevance of steroidal modulators of hormone receptors and anti-cancer cytotoxic steroids10–12,16–18,25,26, herein we have summarised the key advancements made over the past decade (2014–2024) in the discovery and development of anti-cancer steroids that act as enzyme inhibitors, shedding light on their mechanisms of action, rational medicinal chemistry design, and clinical applications. This evidence concerns the gene NR4A1 and cancer.