Abstract: Vasoactive intestinal peptide(VIP)is a peptide hormone containing 28 amino acid residues, and it belongs to glucagon-secretin family.VIP regulates the proliferation and differentiation of normal and cancer cell through the mediation of vasoactive intestinal peptide receptor(VIPR).Different types of cancer cell membrane express distinct density and affinity of VIPR, which provides the underlying molecular basis for labeling VIPR for radionuclide imaging and targeted therapy.The progress of VIPR radioligand research greatly promotes tumor VIPR imaging and therapy.The research will play an important part in the early diagnosis, staging, and targeted therapy of cancer.