Excessive alcohol consumption can seriously threaten the human health. Alcohol dehydrogenase (ADH), as the crucial alcohol metabolizing enzyme, plays an important role in improving alcohol metabolisms within the human body. Food-derived bioactive peptides, as natural product factors with potentials in regulation of body metabolism, can exhibit diverse bioactivities according to their compositions and amino acid sequences. As a result, bioactive peptides have received increasing research attention, specifically regarding their roles in activating ADH activity and modulating alcohol metabolism. Nevertheless, few academic reviews have summarized the current understanding and discussed existing knowledge gaps of food-derived ADH activating peptides. Therefore, in this review, the preparation, isolation, purification, and identification approach of ADH activating peptides are preliminarily summarized. More importantly, the structure-activity relationship and specific action mechanism of ADH activating peptides are also critically discussed. Meanwhile, the potential limitations of the existing studies are also explicitly pointed out in order to provide theoretical references for future research on the ADH activating peptides.