The interest in biological peptides from Arthrospira sp. (syn Spirulina) is increasing due to its GRAS status, the high concentration of proteins and the history of its use as a supplement and nutraceutical agent. Arthrospira peptides can be generated by controlled hydrolysis of the proteins, using proteases, followed by fractionation. The peptides obtained have a range of therapeutic effects. Amongst these bioactive peptides, three classes are of major importance: the antihypertensive (AHP), antimicrobial (AMP) and anticancer (ACP) peptides. AHPs have the ability to work as inhibitors of ACE, the angiotensin-converting enzyme, and help to control several diseases such as hypertension, obesity, and cardiovascular issues. AMPs play a crucial role in the immune response, inhibiting the development of pathogens such as bacteria, fungi, viruses and others. ACPs can aid in tumor control by induction of apoptosis, necrosis, or inhibition of the angiogenesis. Thus, bioactive peptides are of great significance to the pharmaceutical industry. However, they can show secondary effects. This paper reviews the inhibition mechanism of antimicrobial, hypertensive and anticancer peptides from Arthrospira sp., and the possible structures of the peptides according to the type of activity and its intensity. In addition, this paper describes the purification methods, absorption mechanisms, and reviews databases for designing peptides.