Abstract: Survivin is a member of the inhibitor of apoptosis protein family, which plays a key role in tumor apoptosis and angiogenesis pathways. Survivin is overexpressed in a variety of tumor tissues but is hardly expressed in normal terminally differentiated adult tissues, and is closely related to poor prognosis and drug resistance of tumors. Therefore, inhibiting the Survivin protein has become a new strategy for treating cancer and overcoming the drug resistance of tumor cells. This article reviews the mechanism of action and biological functions of Survivin, and elucidates the latest research progress and challenges of Survivin inhibitors. It is of great significance for in-depth understanding and the development of highly selective small molecule inhibitors targeting Survivin.