Nowadays, the search for food-suitable plant proteins is a great challenge. In addition to their sustainability and nutritional value, the focus is more and more on possible positive interactions with human health. To date, the presence of bioactive peptides encrypted in the structure of protein opens new perspectives, addressing the food industry’s request for new ingredients with technological properties and also the nutraceutical and pharmaceutical sectors based on multifunctional health applications. Lupinus is a sustainable genus of the legume family Fabaceae, and the lupin seed-derived bioactive peptides have demonstrated different effects including anti-inflammatory, antidiabetic, antioxidant, antibacterial, hypocholesterolemic, and antihypertensive activities. This review aims to discuss the current knowledge on lupin protein and their bioactive peptides, highlighting the documented health claims, but also the possibility of allergenicity and the work to be done for the development of new functional products.