Emanuele Fabbrizi, Francesco Fiorentino, Antonello Mai, Dante Rotili
INTRODUCTION: Sirtuins have gained significant prominence in scientific research due to their involvement in a wide array of biological processes, including DNA repair, genome stability, transcription modulation, and signal transduction. Dysregulation of their function has been implicated in various pathologies, including cancer, where sirtuins exhibit context-dependent effects. Consequently, the development of sirtuin inhibitors and activators remains an exceptionally important field of research, focusing on the design of selective modulators targeting individual sirtuin isoforms. AREAS COVERED: This review includes the patents regarding sirtuin modulators released from 2020 to 2024 and provides a concise overview of the most relevant modulators developed so far. Relevant patents were systematically identified through comprehensive searches in PubMed (https://pubmed.ncbi.nlm.nih.gov), Google Patents (https://patents.google.com), and Espacenet (https://worldwide.espacenet.com). EXPERT OPINION: Sirtuin modulators are pivotal in addressing aging, metabolism, cancer, and neurodegeneration. Sirtuins regulate key cellular processes like DNA repair, genome stability, and mitochondrial function. Activators show promise in mitigating many age-related diseases such as type 2 diabetes and neurodegeneration. Inhibitors demonstrate efficacy in oncology and neurodegenerative conditions. Advances in PROTAC technology enable selective degradation of specific isoforms, enhancing therapeutic precision. With progress in drug design and high-throughput screening, sirtuin modulators hold immense potential to revolutionize treatments for complex medical challenges.