Background: The growing emphasis on preventative healthcare has driven interest in food-derived bioactive peptides (BAPs) for the treatment of a wide range of diseases. These molecules can potentially promote human health through dietary interventions; however, their full capabilities have not yet been fully realized. Recent innovations and ongoing research are continuously expanding the use of BAPs. Scope and approach: This review explores the preventive potential of BAPs against a wide range of diseases, and their sources, extraction methods, and applications. It critically analyzes preclinical and clinical trial outcomes while acknowledging existing challenges associated with BAPs research and commercialization. Key findings and conclusions: Food-derived BAPs show promise as functional food ingredients, nutraceuticals, and therapeutic agents with diverse bioactivities including antihypertensive, antioxidant, antimicrobial, and immunomodulatory effects. Challenges in BAP research include sourcing, yield, stability, bioaccessibility, bioavailability, and regulatory hurdles. Advancements in peptide discovery through peptidomics, metagenomics, and genome mining, with preparation methods and AI-powered prediction tools offer potential solutions. Emerging technologies such as quantitative systems, pharmacology models, virtual patients, and digital twins may improve the efficiency of predicting drug efficacy and safety potentially facilitating the translation of BAPs from laboratory research to clinical applications. These advances can pave the way for developing personalized nutrition and precision medicine, offering tailored therapeutic strategies to promote human health.