Tinospora cordifolia (Menispermaceae) is an Ayurvedic medicinal plant distributed throughout the Indian subcontinent and China. The whole plant is used in folk and the Ayurvedic system of medicine alone and in combination with other plants. Due to its commercial importance, T. cordifolia has been of intense research interest for the last four decades with the isolation of diverse compounds such as alkaloids, sesquiterpenoids, diterpenoids, phenolics, steroids, aliphatic compounds and polysaccharides, along with the discovery of a wide spectrum of pharmacological properties like immunomodulation, anticancer, hepatoprotective and hypoglycemic. Although pharmacological activities of extracts and compounds of T. cordifolia have been studied both in vitro and in vivo, only few mechanisms of action have been explored and need further elaboration. In the present review, the pharmacological activities of compounds and different extracts of T. cordifolia are highlighted, along with those of the marketed products, showing the relevance of phytochemicals and the standardization of the marketed products for medicinal use. This compilation of the extensive literature of T. cordifolia here will be a referral point for clinical study and the development of standardized phytomedicines in healthcare.