Abstract: Targeted alpha therapy (TAT) is a kind of nuclear medicine treatment based on alpha-emitting radionuclides and tumor-selective carrier molecules for targeted cancer cells. Due to its strong toxicity to targeted cancer cells and relatively less toxic to normal tissues, TAT has been a promising tumor treatment method. Attributed to its suitable half-life (9.9 d), unique decay properties (decay produceing 4α+2β particles), and suitable coordination, ²²⁵Ac has become one of the best choice for α nuclides in TAT. Studies have shown that the targeted ²²⁵Ac-radiopharmaceuticals exhibit excellent effectiveness on cancer treatment, but the preparation of ²²⁵Ac is facing research difficulties. This article summarized the properties of ²²⁵Ac nuclide, the status of the preparation process and ²²⁵Ac-radiopharmaceuticals for TAT. And prospects were proposed for the production process of ²²⁵Ac and its medical application. It is expected that the large-scale production of medical ²²⁵Ac will be standardized, and ²²⁵Ac-radiopharmaceuticals will be approved for tumor treatment in the future.