The article reviews the current status and future perspectives of alpha-emitting radionuclides in targeted endoradiotherapy. Alpha emitters, with their unique physical properties, offer significant advantages in treating single tumor cells due to their high linear energy transfer (LET) and short range in tissue. The review discusses the production of alpha-emitting isotopes, their chemical combination with carrier molecules, and clinical experiences from compassionate use reports and clinical trials. Actinium-225 (225Ac) is highlighted as a critical radionuclide due to its high demand and limited availability, primarily sourced from uranium-233 waste. Alternative production routes, such as cyclotron and reactor production, are explored to address the shortage. Matched radionuclide pairs, including diagnostic and therapeutic isotopes, are discussed, emphasizing the importance of pharmacokinetic properties and tumor target availability. The article also covers the use of carrier molecules for selective delivery, such as monoclonal antibodies and peptides, and provides an overview of clinical applications, including the use of radium-223 in metastatic castration-resistant prostate cancer and bismuth-213 in hematologic diseases. Future perspectives include the integration of imaging and advanced analysis techniques, as well as the potential for synergistic effects with other therapies.The article reviews the current status and future perspectives of alpha-emitting radionuclides in targeted endoradiotherapy. Alpha emitters, with their unique physical properties, offer significant advantages in treating single tumor cells due to their high linear energy transfer (LET) and short range in tissue. The review discusses the production of alpha-emitting isotopes, their chemical combination with carrier molecules, and clinical experiences from compassionate use reports and clinical trials. Actinium-225 (225Ac) is highlighted as a critical radionuclide due to its high demand and limited availability, primarily sourced from uranium-233 waste. Alternative production routes, such as cyclotron and reactor production, are explored to address the shortage. Matched radionuclide pairs, including diagnostic and therapeutic isotopes, are discussed, emphasizing the importance of pharmacokinetic properties and tumor target availability. The article also covers the use of carrier molecules for selective delivery, such as monoclonal antibodies and peptides, and provides an overview of clinical applications, including the use of radium-223 in metastatic castration-resistant prostate cancer and bismuth-213 in hematologic diseases. Future perspectives include the integration of imaging and advanced analysis techniques, as well as the potential for synergistic effects with other therapies.