The increased understanding of the roles tankyrases play in cancer progression has led to the development of an expanding collection of low molecular weight inhibitors suitable for preclinical characterization and more recently to compounds with improved pharmacokinetic properties for potential clinical use, of which three have entered clinical trials namely, stenoparib (Plummer et al. 2020), JPI547 (NCT04335604), and STP06−1002 (NCT04505839) (Kim et al. 2022). The gene discussed is TNKS; the disease is cancer.