Black pepper (Piper nigrum L.) is a tropical plant, best known for its fruit, used as a spice all around the world. The fruits of black pepper can be processed in various ways, so there are end products such as white, black, red, and green pepper. Black pepper contains many substances such as terpenes, alkaloids, lignans, phenylpropanoids, etc., which are responsible for some of the most important biological activities: antioxidant, antimicrobial, anticancer, anti-inflammatory, analgesic, antipyretic, hepatoprotective, bio-enhancing and enzyme inhibitory activities. These activities have also been proven in clinical studies, and probably the future of black pepper research should be based on discovering the most effective way to use the active compounds of pepper for the development of herbal drugs with fewer contraindications than standard drugs. Further preclinical and clinical studies are needed to prepare and apply phytoformulations based on the black pepper isolates.