Microalgae and cyanobacteria have sparked a lot of interest due to their potential in various industries like biorefineries, biopharmaceuticals, food supplements, nutraceuticals, and other high-value products. Polysaccharides, vitamins, proteins, enzymes, and steroids are valuable products isolated from microalgae and cyanobacteria and potentially used in health and biomedical applications. Bioactive compounds derived from microalgae and cyanobacteria exhibit various pharmaceutical properties like antibacterial, anticancer, antiviral, antialgal, and antioxidant. From the properties listed above, the research for novel antibiotics has become particularly appropriate. In addition, the possible emergence of resistance against pathogens, as well as the potential decline in antibiotic efficacy, has prompted researchers to look for a new source of antibiotics. Microalgae and cyanobacteria have indicated a great and unexplored potential among these sources. For this reason, microalgae and cyanobacteria have been highlighted for their efficiency in different industrial sectors, as well as for their potential uses in the betterment of human and environmental health. This review gives an overview of bioactive compounds and metabolites with several biological properties isolated from microalgae and cyanobacteria for treating different animal and human diseases.