Background: Plants have been known as an integral part of traditional medicine because of their phytoconstituents with their miraculous substances. Tinospora cordifolia (Guduchi/ Giloy) is one such plant having pharmacological functions and medicinal values due to its several constituents such as terpenes, glycosides, alkaloids, steroids and flavonoids. Thus, it has been rightly mentioned in old texts as “Amrita”.Objective: The objective of the present review is to extend the current knowledge, importance and beneficial pharmacological applications of guduchi in humans for safeguarding various health issues. Methods: We extensively reviewed, analyzed and compiled salient information from the published literature available in PubMed and other scientific databases. Results: The present review describes medicinal applications of T. cordifolia in countering various disorders and usages as anti-oxidant, anti-hyperglycemic, antihyperlipidemic, hepatoprotective, cardiovascular protective, neuroprotective, osteoprotective, radioprotective, anti-anxiety, adaptogenic agent, analgesic, anti-inflammatory, antipyretic, a thrombolytic agent, anti-diarrheal, anti-ulcer, anti-microbial and anti-cancer agent. The plant is also a source of micronutrients viz. copper, calcium, phosphorus, iron, zinc and manganese. A special focus has been made on its health benefits in treating endocrine and metabolic disorders and its potential as an immune booster. Several patents have been filed and granted to inventions encompassing T. cordifolia as a major component of therapeutics for ameliorating metabolic, endocrinal and several other ailments, aiding in the betterment of human life expectancy. Conclusion: The information presented would be beneficial for researchers, medical professionals and pharmaceutical companies to design and develop effective medicines, drugs and healthical products exploiting the multiple as well as specific modes of actions of T. cordifolia, and also help in promoting and popularizing this rich herb having promising potentials to prevent and treat various ailments.