Eurycoma longifolia Jack (E. longifolia) is a well-recognized traditional herbal medicine that offers a wide dynamic range of biomedical applications including anti-osteoporotic, anticancer, anti-proliferative, anti-malarial, antimicrobial, antioxidant, aphrodisiac, anti-inflammatory, anxiolytic, anti-diabetic, anti-rheumatism and anti-ulcer properties. This review aims to overview the pharmacokinetic and a pharmacodynamic algorithm of E. longifolia and its bioactive components. Analysis of pharmacokinetic profile revealed that E. longifolia exhibit higher bioavailability, high volume of distribution, slow elimination rate, and does not show inhibitory effects on cytochrome P450 isoenzymes. E. longifolia has been used, alone or in combination with other pharmacological agents, in the form of crude extracts, standard extracts, or decoctions of different plant parts (i.e., herbs, shrubs, stem, leaves, and roots) for the treatment of various ailments in animals and humans. Among various bioactive constituents, eurycomanone has been found to be the most remarkable, super-stable, versatile, and most potent phytochemical (isolated or extracted from root extracts) against various types of animals and human diseases. Based on its well-established pharmacokinetic and pharmacodynamic profiles, we suggested that E. longifolia can be a well-accepted complementary and altative medicine for the treatment of different types of human ailments.