Milk is a good source of bioactive peptides of high nutritive/ pharmaceutical value. In recent decades, the curiosity about bioactive milk peptides has been increasing because of their positive impact on physiological and metabolic functions in human health. A variety of naturally acquired bioactive peptides have been found in fermented dairy products like sour milk and cheese. Initially, these bioactive peptides are found as inactive forms within the precursor protein sequence and can be released in different ways. They can be generated by gastrointestinal digestion of milk, fermentation of milk with proteolytic microorganisms, or hydrolysis via proteolytic enzymes. Once they are released from the precursor protein sequence, they influence body functions and human health. Peptides derived from cow milk exert multifunctional properties, including antimi-crobial, antidiabetic, antihypertensive, anti-inflammatory, immune-modulatory, antioxidant activ-ities, etc. Bioactive antimicrobial peptides are observed in the Cow milk proteins. The Cow milk peptides afford the non-immune-based defense and control for various microbial infections. These activities depend upon their amino acid composition/ sequence. Potential pathogens are con-stantly exposed to mucosal surfaces (lungs and small intestine). The risk of chronic disease was inhibited by antimicrobial peptides, which may afford natural immune protection with the avoid-ance of microbial resistance. In this regimen, the present review summarizes the milk-derived an-timicrobial peptides obtained from casein/ whey protein, along with their future perspectives in the pharmaceutical and dairy industries.