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Since the discovery of aptamer, aptamer has become an exciting and promising diagnostic and therapeutic tool because of its excellent targeting selectivity, high potential affinity, simple modification, scalability, flexibility, low immunogenicity and a wide range of drug delivery platforms. Targeted therapy is the frontier research of modern medicine on countless clinical diseases. Aptamer is the focus of biological targeting research, especially tumor research. They not only have high clinical application potential in tumor targeted detection, but also have high application prospects in tumor therapy as targeted tumor drug carriers. In this review, we summarize the progress of aptamers in imaging technology and targeted therapy. We will focus on aptamer based targeted therapy, using aptamers as biotechnology tools and targeted therapeutic agents for targeted drug delivery.