Tagitinin C, an important sesquiterpene lactone derived from Tithonia diversifolia, has exhibited multiple biological actions. T. diversifolia is a widely used ethnomedicinal plant for treating a wide range of diseases due to its biochemical components, primarily sesquiterpenes. Treatments such as radiation, surgery, immunotherapy, and chemotherapy employed on cancer patients have an impact not only on cancer cells but also affects normal cells. Despite the available conventional cancer treatments, phytocompounds based treatment less harmful and less toxic alternatives need to be explored. Tagitinin C, a sesquiterpene lactone has shown inhibition against various tumors and cancer cell lines. This review delves into the therapeutic effects of the bioactive compound Tagitinin C against different cancers and tumors and the future prospects in the medical and pharmaceutical sectors. A Comprehensive study from scientific databases, such as Pubmed, Web of Science, Google Scholar, Sci-Finder, etc., was scrutinized to collect the relevant information. Detailed insights on the mechanism of action and compound interaction with cancer cell lines were collated and presented. This review summarizes the pharmacological properties of Tagitinin C and the action potential as well. (c) 2024 SAAB. Published by Elsevier B.V. All rights are reserved, including those for text and data mining, AI training, and similar technologies.