Bioactive peptides derived from milk proteins are of particular interest to the food industry due to the potential functional and physiological roles that they demonstrate, particularly in relation to cardiovascular disease (CVD). By 2020 it is estimated that heart disease and stroke will become the leading cause of death and disability worldwide. Acute and chronic cardiovascular events may result from alterations in the activity of the renin-angiotensin aldosterone system and activation of the coagulation cascade and of platelets. Medications that inhibit angiotensin converting enzyme (ACE) are widely prescribed in the treatment and prevention of cardiovascular disease. ACE inhibitory peptides are of particular interest due to the presence of encrypted inhibitory peptide sequences. In particular, Ile-Pro-Pro and Val-Pro-Pro are fore runners in ACE inhibition, and have been incorporated into commercial products. Additionally, studies to identify additional novel peptides with similar bio-activity and the ability to withstand digestion during transit through the gastrointestinal tract are ongoing. The potential sources of such peptides in cheese and other dairy products are discussed. Challenges to the bio-availability of such peptides in the gastro intestinal tract are also reviewed. Activation of platelets and the coagulation cascade play a central role in the progression of cardiovascular disease. Platelets from such patients show spontaneous aggregation and an increased sensitivity to agonists which results in vascular damage and endothelial dysfunction associated with CVD. Peptide sequences exhibiting anti-thrombotic activity have been identified from fermented milk products. Studies on such peptides are reviewed and their effects on platelet function are discussed. Finally the ability of food derived peptides to decrease the formation of blood clots (thrombi) is reviewed. In conclusion, due to the widespread nature of cardiovascular disease, the identification of food derived compounds that exhibit a beneficial effect in such widespread areas of CVD regulation will have strong clinical potential. Due to the perception that food derived products have an acceptable risk profile they have the potential for widespread acceptance by the public. In this review, selected biological effects relating to CVD are discussed with a view to providing essential information to researchers.