Background:The plants belonging to the genus Cinnamomum traditionally used as an ethnomedicine in Asia, Europe, and North America. Cinnamomum osmophloeum Kanehira, is an endemic and economic medicinal plant of Taiwan. It is traditionally used as an antibacterial, antifungal, anti-termite, antidiabetic, anti-hyperuricemia, antiinflammatory, and antioxidant agent. Despite these attributes, C. osmophloeum is not enough explored scientifically. This review updated the essential oils and other secondary metabolites, and the pharmacological activities of C. osmophloeum, as well as its other economic benefits. Methods: The information in the review is extracted from the major scientific databases, such as PubMed, BioMed Central, Google scholar, Elsevier, ACS publications, MDPI, Taylor and Francis, Wiley Online Library, Scopus, Springer, and Web of Science, using journals, dissertations, books and/or chapters, and conference proceedings. Results: Various secondary metabolites including essential oil components, flavonoids, lignans, and benzenoids are reported from the extracts of C. osmophloeum. The review established a wide range of pharmacological properties including, antibacterial, antidiabetic, anti-fungal, anti-inflammatory, antioxidant, antitermitic, anti-tyrosinase, anti-xanthine oxidase, anxiolytic, cytotoxic, hepatoprotective, and mosquito larvicidal properties of extracts, as well as essential oils and other secondary metabolites of C. osmophloeum. Conclusions: The present review provides a scientific basis for future studies and necessary information for the development of C. osmophloeum based therapeutic agents.