Abstract: ³H and ¹⁴C labeled compounds have many advantages as the tracer such as long half-life, low radioactive energy, low toxicity and high detection sensitivity. They are widely used in biotechnology, pharmaceutical development, agriculture, industry and many other fields. The demand for ³H and ¹⁴C labeled compounds is increasing with the development of new drug research. In the present paper, the summarizes of the preparation methods of ³H and ¹⁴C labeled compounds was performed and the analysises of their applications in various research fields were described. A brief review of the development of ³H and ¹⁴C labeled compounds in China and prospects of the domestic radiolabeled compounds development were performed in this paper too. All these works were hoped to promote the development of labeled compounds and meet the needs of domestic scientific research for labeled compounds.