For all these reasons, in the last years, USP‐7 has emerged as a novel and exciting therapeutic target for cancer treatment, and several covalent and noncovalent small‐molecule inhibitors have been developed with promising efficacy in preclinical studies.[15, 16, 17, 18, 19, 20, 21, 22, 23] Particularly, monocycles (e.g., thiazoles and pyridines) or bicyclic (e.g., quinazolines, pyrazolo‐pyrimidines, thieno‐pyrimidines, and imidazo‐triazines) and tricyclic derivatives (e.g., triterpenoid derivatives) have been recently published and patented.[16]. This evidence concerns the gene USP7 and cancer.