Tinospora cordifolia is a deciduous climbing shrub described as ‘the one who protects the body against diseases’. It is one of the most versatile rejuvenating shrub also known as ‘Giloya’ in Indian vernacular having many therapeutic applications. The pharmaceutical significance of this plant is mainly because of the leaves, barks and roots contain various bioactive compounds such as alkaloids, glycosides, lactones, steroids, polysaccharides and aliphatic compounds having various medicinal importance viz. immunomodulatory or immunostimulatory, antitumor, cognition, antiinflammatory, anti-neoplastic, antihyperglycemia, antihyperlipidemia, antioxidant, antituberculosis, gastrointestinal and hepatoprotection, anti-osteoporotic, anti-angiogenic, antimalarial, anti-allergic and side effects prevention of the cancer chemotherapy. The bitter principles present in the leaves, stems, roots and barks viz. tinosporine, tinosporide, tinosporaside, cordifolide, cordifol, berberine, cordifolioside A, B, C, amritosides A, B, C and columbine which act as therapeutic agents and play vital role in many therapeutic applications. The climbing shrub has shown a great potential for the development of industrial products and commercial exploitation of biopharmaceuticals for the treatment of various diseases. The focus of the present review is to galvanize the potential of medicinal importance of this shrub for health care management. However, there are currently no standard protocols for guaranteeing its product for quality and efficacy. From a pharmacological point of view, safety is a relative concept and it should be clear by further appropriate research in this direction. A systematic research should be undertaken to develop a modern drug using compounds isolated from this climbing shrub. A modern effective and safe drug can be developed after extensive investigation of its pharmacodynamics, kinetics, proper standardization and clinical trials.