Cantharidin is an antineoplastic drug that can be extracted from cantharis or artificially synthesized.However,clinical application of cantharidin is limited because of its strong toxicity.Synthetic cantharidin derivatives such as norcantharidin,sodium cantharidate,sodium demethylcantharidate and methylcantharidinimide,have notable curative effects with low toxicity.In this paper,research progress on the antitumor activities and molecular mechanisms of cantharidin and its derivatives was summarized,in order to make full use of the traditional Chinese medicine resources.