Abstract: Polyamide-amine is a kind of widely studied dendrimer with the characteristics of controllable particle size, good monodispersity, non-immunogenicity, biodegradablility and easy modification on the surface. After various modifications, polyamide-amines have the advantages of controllable drug release, good targeting, low toxicity and so on, and have been widely applied in tumor-targeted drug delivery system. In this paper, the recent advances in the research of polyamide-amine dendrimers as tumor-targeted drug delivery systems were reviewed.