Currently an ample interest is found among oncologists to explore anticancer compounds from herbs. Sesquiterpene lactones have accredited significant attention in pharmacological research. Costunolide is a well-known sesquiterpene lactone present in plants used as popular herbal remedy. Several plant-derived compounds are currently successfully employed in cancer treatment. Growing evidences demonstrated that costunolide possesses anticancer activities by inhibiting cell proliferation, tumor invasion, angiogenesis, metastasis and inducing apoptosis of a variety of tumor cell lines. This review is aimed to summarize the recent researches about costunolide focusing on anti-tumor activity and to lay emphasis on its molecular targets and its mechanisms, which may help the further design and conduct of preclinical and clinical trials.