Abstract: Tyrosol (Ty) and its derivatives have gathered considerable attention in recent years due to their diverse pharmacological properties and potential therapeutic applications. This comprehensive review aims to summarize the current understanding of the therapeutic potential of Ty and its derivatives in combating various diseases, including cancer, cardiovascular disease (CVD), neurodegenerative diseases, diabetes, and obesity. This review highlights the multifaceted properties of Ty, including its pharmacokinetic profile and pharmacological actions, which contribute to its efficacy against these prevalent health conditions. Moreover, the antimicrobial and wound-healing effects of Ty are explored, elucidating its potential for broader therapeutic utilization. While existing studies provide evidence supporting the beneficial effects of Ty, gaps remain in our understanding of its molecular mechanisms of action and the exploration of novel derivatives. Future research efforts are thus critical for unraveling the full therapeutic potential of Ty and its derivatives. Moreover, the synthesis of novel derivatives with enhanced efficacy and improved bioavailability shows potential for addressing unmet medical needs. This review emphasizes the necessity for ongoing research into Ty and its derivatives, providing valuable insights into their potential as essential therapeutic agents for addressing diverse health conditions.