Abstract: Targeted alpha therapy(TAT) is a very promising therapeutic way for the treatment of cancers. In TAT, a radiopharmaceutical containing alpha-emitter radionuclide was used to deliver systemic radiation selectively to cancer cell while minimizing systemic toxic effects. In comparison to β-particle, α-particle has higher energy, higher linear energy transfer(LET) and a shorter penetration range in tissues. Therefore, TAT has distinct advantages for use in targeted therapy. In this review, some actinoid elements and the radiometallic decay daughters of these actinoid elements, used in TAT, were discussed. These radiometallic nuclides included ²²⁵Ac, ^212/213Bi, ²¹²Pb, ²²⁷Th and ²²³Ra. Firstly, the physical, radiobiological properties of α-particle and β-particle were compared. Secondly, the chemical properties and their source of these radiometallic nuclides were described. Thirdly, the selected bifunctional chelators of TAT radiopharmaceuticals were presented. Fourthly, the current status of TAT radiopharmaceuticals was introduced. Lastly, our views about the future challenges and prospects of TAT radiopharmaceuticals were given.