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ETHNOPHARMACOLOGICAL RELEVANCE Glycosmis pentaphylla (Retz.) DC. is a perennial shrub indigenous to the tropical and subtropical regions of India, China, Sri Lanka, Myanmar, Bangladesh, Indonesia, Malaysia, Thailand, Vietnam, Philippine, Java, Sumatra, Borneo and Australia. The plant is used extensively within these regions as a traditional medicine for the treatment of a variety of ailments including cough, fever, chest pain, anemia, jaundice, liver disorders, inflammation, bronchitis, rheumatism, urinary tract infections, pain, bone fractures, toothache, gonorrhea, diabetes, cancer and other chronic diseases. AIM OF THE REVIEW This review aims to present up-to-date information regarding the taxonomy, botany, distribution, ethnomedicinal uses, phytochemistry, pharmacology and toxicological profile of G. pentaphylla. The presented information was analyzed critically to understand current work undertaken on this species and explore possible future prospects for this plant in pharmaceutical research. MATERIALS & METHODS Bibliographic databases, including Google Scholar, PubMed, Web of Science, ScienceDirect, SpringerLink, Wiley Online Library, Semantic Scholar, Europe PMC, Scopus, and MEDLINE, were explored thoroughly for the collection of relevant information. The structures of phytoconstituents were confirmed with PubChem and SciFinder databases. Taxonomical information on the plant was presented in accordance with The Plant List (version 1.1). RESULTS Extensive phytochemical investigations into different parts of G. pentaphylla have revealed the presence of at least 354 secondary metabolites belonging to structurally diverse classes including alkaloids, amides, phenolic compounds, flavonoids, glycosides, aromatic compounds, steroids, terpenoids, and fatty derivatives. A large number of in vitro and in vivo experiments have demonstrated that G. pentaphylla had anticancer, antimutagenic, antibacterial, antifungal, anthelmintic, mosquitocidal, antidiabetic, antihyperlipidemic, anti-oxidant, anti-inflammatory, analgesic, antipyretic, anti-arsenicosis, and wound healing properties. Toxicological studies have established the absence of any significant adverse reactions and showed that the plant had a moderate safety profile. CONCLUSIONS G. pentaphylla can be suggested as a source of inspiration for the development of novel drugs, especially anticancer, antimicrobial, anthelmintic, and mosquitocidal agents. Moreover, bioassay-guided investigations into its diverse classes of secondary metabolites, especially the large pool of nitrogen-containing alkaloids and amides, promises the development of novel drug candidates. Future pharmacological studies into this species are also warranted as many of its traditional uses are yet to be validated scientifically.