Abstract: Alpha-emitting radionuclides provide effective cellkilling properties in vivo and have been shown to be effective in cancer treatment. Its short-range make little effect on normal tissues, thus alpha-emitting radionuclides drugs is one of the important research focus areas and radiopharmaceutical research. The excellent nature of the radionuclide (right half life, ray energy, etc.), stable supply of high purity nuclides, suitable radionuclide carrier base and excellent kinetics in vivo are necessary to the production and research of alpha-emitting radionuclides. At present, the alpha-emitting radionuclides include ²²³Ra, ²²⁵Ac, ²¹³Bi, ²¹¹At, ²¹²Bi, ¹⁴⁹Tb and ²²⁷Th were investagated. The preparation and sources of the above radionuclides and the latest developments for targeted cancer therapy were described. The existing problems, status and clinical application were briefly discussed.