Cyanobacteria have attracted the attention of researchers because of their promising role as primary and secondary metabolites in functional food and drug design. Due to an ever-increasing awareness of health and the use of natural products to avoid the onset of many chronic and lifestyle metabolic diseases, the global demand for the use of natural drugs and food additives has increased in the last few decades. There are several reports about the highly valuable cyanobacterial products such as carotenoids, vitamins, minerals, polysaccharides, and phycobiliproteins showing antioxidant, anti-cancerous, anti-inflammatory, hypoglycemic, and antimicrobial properties. Recently, it has been shown that allophycocyanin increases longevity and reduces the paralysis effect at least in Caenorhabditis elegans. Additionally, other pigments such as phycoerythrin and phycocyanin show antioxidative properties. Because of their high solubility in water and zero side effects, some of the cyanobacterial tetrapyrrole derivatives, i.e., pigments, facilitate an innovative and alternative way for the beverage and food industries in place of synthetic coloring agents at the commercial level. Thus, not only are the tetrapyrrole derivatives essential constituents for the synthesis of most of the basic physiological biomolecules, such as hemoglobin, chlorophyll, and cobalamin, but also have the potential to be used for the synthesis of synthetic compounds used in the pharmaceutical and nutraceutical industries. In the present review, we focused on the different aspects of tetrapyrrole rings in the drug design and food industries and addressed its remaining limitations to be used as natural nutrient supplements and therapeutic agents.