The major cancer therapeutic modalities include surgery, chemotherapy and radiotherapy. Although these treatment regimens have played a significant role in effectively inhibiting cancer, their associated morbidity reduces the overall quality of life. Thus, researchers are striving to identify any alternate therapeutic approach capable of inhibiting cancer without eliciting the added morbidity. Among the alternate cancer therapeutics being researched, much importance is being given to the use of plants due to the presence of a wide variety of anti-carcinogenic compounds. Tinospora cordifolia (Tc) is one such plant and has shown to exhibit anti-carcinogenic properties. The present review aimed to systematically analyze published data on the effect of Tinospora cordifolia-derived phytocomponents on cancer. PubMed, Scopus, Web of Science, Embase and Cochrane library were searched using the keywords Tinospora cordifolia; anticancer; phytocomponents until March 20, 2019. In vivo and in vitro original studies in the English language were included. Of the 342 articles identified, only 25 articles met the selection criteria and were included in the review. Significant anti-carcinogenic properties were exhibited by Tinospora cordifolia-derived phytocompounds including palmative, berberine, new clerodane furanoditerene glycoside, arabinogalactan, phenolic compounds and epoxy cleodane diterpene. No significant side effects have been elicited with its use. Based on the data from the included studies, Tinospora cordifolia could be a natural therapeutic agent for cancer, provided its anti-carcinogenic properties can be elicited consistently at a large scale in clinical trials.