Fucoxanthin, a carotenoid widely studied in marine microalgae, is at the heart of scientific research because of its promising bioactive properties for human health. Its unique chemical structure and specific biosynthesis, characterized by complex enzymatic conversion in marine organisms, have been examined in depth in this review. The antioxidant, anti-inflammatory, and anti-cancer activities of fucoxanthin have been rigorously supported by data from in vitro and in vivo experiments and early clinical trials. Additionally, this review explores emerging strategies to optimize the stability and efficacy of fucoxanthin, aiming to increase its solubility and bioavailability to enhance its therapeutic applications. However, despite these potential benefits, challenges persist, such as limited bioavailability and technological obstacles hindering its large-scale production. The medical exploitation of fucoxanthin thus requires an innovative approach and continuous optimization to overcome these barriers. Although further research is needed to refine its clinical use, fucoxanthin offers promising potential in the development of natural therapies aimed at improving human health. By integrating knowledge about its biosynthesis, mechanisms of action, and potential beneficial effects, future studies could open new perspectives in the treatment of cancer and other chronic diseases.