Tinospora cordifolia (Giloy) is a medicinal plant used in folk and Ayurvedic medicines throughout India since ancient times. All the parts of the plant are immensely useful due to the presence of different compounds of pharmaceutical importance belonging to various groups as alkaloids, diterpenoid lactones, glycosides, steroids, sesquiterpenoid, and phenolics. These compounds possess pharmacological properties, which make it anti-diabetic, antipyretic, anti-inflammatory, anti-oxidant, hepato-protective, and immuno-modulatory. However, due to the increasing population, there is an inadequate supply of drugs. Therefore, this review focuses on phytochemistry, ethnopharmacology, clinical application and its conservation strategies so that the plant can be conserved for future generations and utilized as alternative medicine as well as to design various pharmacologically important drugs.