Background: Pittosporum (the family Pittosporaceae) contains flowering plants, which was used as folk medicines in some countries of Asia, Europe, and Africa. Traditional use and pharmacological values of plants in this genus were deduced from a great role of their secondary metabolites. Objective: The ultimate goal of the review fully provides significant information on traditional use, phytochemistry, and pharmacology of Pittosporum plants. Methods: The search for reference data is mostly based on electronic resources, such as Google Scholar, Sci-Finder, and Web of Science. “Pittosporum” is the most important keyword, in which it was used alone or combined with other words to seek literature documents. Results: Traditionally, Pittosporum species are on the recommended list for medicinal purposes and fragrance preparation. From the 1960s to the present, more than 270 metabolites have been isolated with the derivatives type terpenoids, saponins, and lignans being the main phytochemical classes. Essential oils derived from Pittosporum species were dominated by terpenoids and fatty acids. Accumulating evidence has firmly revealed that Pittosporum constituents generated a wide variety of pharmacological activities, including cytotoxic, anti-inflammatory, antioxidative, antimicrobial, antiparasitic, antiarrhythmic, antinociceptive, antimalarial, enzyme inhibitory, and hepatoprotective activities. Conclusion: Technological advances in the chromatographic isolation of huge amounts are desirable. Toxicological assessments are needed. In vivo pharmacological experiments, molecular mechanisms of action, and clinical evaluations are warranted.