Cancer is a complex disease involving unregulated cell growth. Cancer remains the leading cause of death over the world. Isoobtusilactone A, a butanolide, has been first isolated from the ripe berries of Lindera benzoin (Lauraceae). Studies have shown that isoobtusilactone A has potential anticancer activity and induces apoptosis in many cancers. This review describes the pharmacological properties of isoobtusilactone A. This review gathers the information from eletronic and scientific literature database such as Pubmed, Medline, ScienceDirect and so on. Isoobtusilactone A has anticancer activity and modulates multiple targets in cancer cells. The review presents the molecular mechanism of action of isoobtusilactone A in cancer cells and provides information for researchers