Aganonerion polymorphum Pierre ex Spire, a plant species belonging to the Apocynaceae family, is predominantly distributed across Southeast Asian countries, such as Vietnam, Thailand, and Laos. Traditionally, this species has been used in folk medicine to treat digestive disorders, inflammation, and fever. Recent studies have shown that A. polymorphum leaves are rich in bioactive compounds, including flavonoids, polyphenols, coumarins, and sterols, which contribute to its antibacterial, antioxidant, anti-inflammatory, and potential anticancer properties. In addition to its medicinal uses, this plant is also employed in Vietnamese cuisine, especially as an aromatic herb in sour soups and traditional dishes in the Mekong Delta region. This review compiles current research on the botanical characteristics, chemical composition, and biological activities of A. polymorphum, as well as its traditional applications and potential uses. Moreover, it proposes future research directions to effectively explore and utilize this native plant for pharmaceutical and food industry purposes.