<p>Auraptene (7-geranyloxycoumarin) a naturally occurring bioactive coumarin geranyl ether is widely distributed across a limited number of plant families, including Rutaceae, Apiaceae, and a few others. Notably, this oxyprenylated coumarin has been extracted from several edible fruits, vegetables, and medicinal plants consumed worldwide. There is growing evidence supporting the therapeutic benefits of this molecule. Auraptene is highly pleiotropic, modulating intracellular signaling pathways that regulate inflammation, cell growth, and apoptosis. It holds potential for preventing and treating various diseases due to its anti-inflammatory and antioxidant activities, along with an excellent safety profile. Particularly in the last three years, this secondary metabolite has been the subject of intense research, with more than 50 articles published during this period. These studies have explored various aspects of auraptene’s pharmacological activities and, for the first time, included clinical trials involving phytopreparations containing this biologically active coumarin. This review aims to provide a comprehensive overview of the data published in the last three years, offering insights into the therapeutic and chemopreventive potential of auraptene.</p>