Tinospora cordifolia (Willd.) Miers, commonly known as Giloy or Guduchi, is a well-recognised medicinal plant in Ayurveda with a long history of therapeutic use. In recent decades, it has gained significant attention in modern biomedical research due to its broad pharmacological potential. This review provides a concise yet comprehensive synthesis of current knowledge on its phytochemical composition, pharmacological mechanisms, clinical relevance, and safety profile. Literature was systematically analysed from databases including PubMed, Scopus, and Web of Science. The plant contains diverse bioactive constituents such as isoquinoline alkaloids (berberine, palmatine), diterpenoid lactones (tinosporide, columbin), glycosides (cordifoliosides), polysaccharides, and phenolic compounds. Experimental studies demonstrate immunomodulatory, antioxidant, anti-diabetic, anti-inflammatory, hepatoprotective, antimicrobial, and neuroprotective effects. Clinical evidence suggests modest benefits in metabolic and inflammatory disorders, although limitations in trial design persist. Safety data indicate general tolerability, with rare reports of hepatotoxicity requiring further investigation. Future research should prioritise standardisation, large-scale clinical trials, and mechanistic validation using advanced technologies. This review provides an updated framework for integrating T. cordifolia into evidence-based medicine.