Chia (S. hispanica L.) is an annual herbaceous plant that has gained popularity for its seeds of high-quality vegetative proteins, richest contents of omega-3 polyunsaturated fatty acids (\mathrm{\Omega }-3 PUFA), soluble dietary fiber, and great gelling ability, as well as its high contents of bioactive peptides of antioxidative and nutraceutical potential for many other clinical biomarkers. Such health protective bioactive peptides should be utilized for supplementation in the food and nutrition industries. This review was therefore designed to align the researches done on chia bioactive peptide’s derivation, processing, consumption and to identify their antioxidative and nutraceutical potential for various disease biomarkers. The evidence gathered is fairly compelling for the health-promising nutraceutical and clinical potential of chia seed bioactive peptides as antioxidants, dipeptidyl peptidase-IV inhibitors (DPP4), angiotensin-converting enzyme (ACE) inhibitors, and anti-inflammatory drugs. Their assimilation into everyday diets has the potential to open new doors in health departments and food sectors.