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.