Background: Cordia myxa L. (CM) is a valuable ethnomedicinal plant from Boraginaceae family. Traditionally, CM parts especially fruits and leaves are used in chest and urinary tract infections, diarrhoea, dysentery, tuberculosis, liver and spleen disorders, chronic fever, malaria etc. Objective: Despite of known importance and uses, CM has gained relatively less attention of researchers and concise reviews revealing the medicinal potential of CM are scanty. The present review summarizes the chemical constituents and biological activities of CM and aims to stimulate future research to develop it as a functional health food. Results: Analysis of literature on CM showed that its fruits are a rich source of nutrients and are frequently employed in wide ailments such as urinary and respiratory tract infections, chronic fever, liver disorders, asthma, used as anthelmintic, diuretic, expectorant and purgative. Scientific studies have shown the antidiabetic, analgesic, anti-inflammatory, anti-cancer, antioxidant, antiplasmodial, hepatoprotective, hypotensive, antiulcer and antimicrobial activities of CM. More than 45 compounds belonging to carbohydrates, steroids, carotenoids, phenols, flavonoids and alkaloids have been reported from various parts of CM. Conclusion: Systematic preclinical studies support the traditional claims of CM. The analysis of available literature showed that CM could be developed as a drug. Further, studies such as detailed pharmacological and toxicological evaluation, isolation of bioactive compounds, quantitative phytochemistry and structure activity relationship are scanty and thus, crucial to be addressed for uplifting the scientific value of this revered medicinal plant.