Crocus sativus L., commonly known as saffron, is a highly valued medicinal plant recognized for its extensive phytochemical richness and diverse biological potentials. This review elucidates the key bioactive compounds, including crocin, picrocrocin, and safranal, which contribute to its therapeutic properties. Saffron exhibits significant antioxidant, anti-inflammatory, and anticancer activities, making it a promising candidate for various health applications. Its historical use in traditional medicine, combined with modern scientific validation, underscores saffron's role as a multifaceted agent in promoting health and combating diseases. Further research is essential to fully harness its medicinal benefits.