Abstract: Radiopharmaceuticals derived from targeted molecules labeled with radioiodine have always been the research hotspots in the field of nuclear medicine. Radioiodine labeling also has a clear application demand in pharmacokinetic research. Methods for radioiodine labeling include direct labeling method and indirect labeling method. Direct labeling method has the advantages of rapid reaction, simple operation and high radiochemical yield, but it has the problems of narrow scope of application and deiodination in vivo; and for the indirect method, although radioiodine labeled drugs shows good stability in vivo, it has the problems as complicated process and low radiochemical yield. With the purpose of providing reference for the development of radioiodine labeled drugs and isotope pharmacokinetics study, this paper introduced the research progress, application scope, advantages and disadvantages of radioiodine labeling methods, and prospected the development of radioiodine labeling methods.