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Abstract Background Cancer is a persistent global health challenge, demanding continuous exploration of innovative therapeutic strategies. Hydroxytyrosol (HT), derived from olive oil, has garnered attention for its potent antioxidant and anti-inflammatory properties, revitalizing interest due to recent breakthroughs in comprehending its intricate anticancer mechanisms. Main Body This review conducts a detailed analysis of hydroxytyrosol’s molecular mechanisms in cancer. Delve into the complex pathways and processes underlying its anticancer properties, including its impact on critical cellular events such as inhibiting cancer cell growth, proliferation, metastasis, and apoptosis. We meticulously evaluate HT efficacy and safety through scrutiny of preclinical and clinical studies. Additionally, we explore the potential synergistic effects of combining HT with conventional cancer therapies to improve treatment outcomes while reducing side effects, offering a comprehensive approach to cancer management. Conclusion This review stands as a valuable resource for researchers, clinicians, and policymakers, providing profound insights into HT potent anticancer activity at the molecular level. It underscores the immense potential of natural compounds in the intricate realm of cancer management and highlights the urgent need for further research to translate these discoveries into effective clinical applications. Ultimately, it fosters the development of targeted and personalized therapeutic approaches, reigniting hope in the ongoing battle against cancer and enhancing the quality of life for those afflicted by this relentless disease.