Tinospora cordifolia, or "guduchi," is a reported medicinal plant of high therapeutic value. Historically, it was utilized in Ayurveda and other herbal medicinal therapies, where it is valued for its efficacy in treating a range of diseases, such as metabolic disorders, infectious diseases, autoimmune diseases, and cancer. This manuscript presents the pharmacological significance of T. cordifolia, where its multi-dimensional bioactive molecules, such as alkaloids, diterpenoid lactones, and steroids, are responsible for its therapeutic actions. Recent scientific studies show its chemopreventive value, especially in regulating cellular proliferation and apoptosis. With the growing interest in the world for plant-based therapeutics, more studies are needed to prove its efficacy, to explain its mechanisms of action, and to determine its potential in today's medicine.