Diosmin, a potent bioflavonoid derived from citrus fruits, has gained significant attention for its anticancer potential, reflecting a critical need in the ongoing battle against cancer. Amidst increasing cancer incidence, the quest for safer and more effective treatments has brought diosmin to the forefront, given its unique pharmacological profile distinct from other flavonoids. Diosmin's anticancer mechanisms are multifaceted, involving apoptosis induction, angiogenesis inhibition, and metastasis prevention. Extensive research encompassing cellular studies, animal models, and limited clinical trials underscores its efficacy not only against cancer but also in managing chronic venous insufficiency and hemorrhoids, attributing to its anti‐inflammatory properties. Furthermore, diosmin exhibits low toxicity and complements conventional chemotherapy, proposing its utility as an adjunct therapy in cancer treatment protocols. The review delves into the specific anticancer advantages of diosmin, distinguishing it from the broader flavonoid category. It provides a detailed analysis of its implications in preclinical and clinical settings, advocating for its consideration in the oncological therapeutic arsenal. By juxtaposing diosmin with other herbal medicines, the review offers a nuanced perspective on its role within the wider context of natural anticancer agents, emphasizing the need for further clinical research to substantiate its efficacy and safety in oncology.