This review summarizes recent progress and developments as well as the most important pitfalls in targeted alpha-particle therapy, covering single alpha-particle emitters as well as in vivo alpha-particle generators. It discusses the production of radionuclides like 211At, 223Ra, 225Ac/213Bi, labelling and delivery employing various targeting vectors (small molecules, chelators for alpha-emitting nuclides and their biomolecular targets as well as nanocarriers), general radiopharmaceutical issues, preclinical studies, and clinical trials including the possibilities of therapy prognosis and follow-up imaging. Special attention is given to the nuclear recoil effect and its impacts on the possible use of alpha emitters for cancer treatment, proper dose estimation, and labelling chemistry. The most recent and important achievements in the development of alpha emitters carrying vectors for preclinical and clinical use are highlighted along with an outlook for future developments.

• Keywords
• 223Ra, actinium, alpha particle, astatine, bismuth, decay, in vivo generators, nuclear recoil, radium, targeted alpha therapy,
• MeSH
• Actinium chemistry   therapeutic use   MeSH
• Alpha Particles therapeutic use   MeSH
• Astatine chemistry   therapeutic use   MeSH
• Bismuth chemistry   therapeutic use   MeSH
• Chelating Agents chemistry   pharmacokinetics   MeSH
• Radiation Dosage MeSH
• Heterocyclic Compounds, 1-Ring chemistry   pharmacokinetics   MeSH
• Heterocyclic Compounds chemistry   pharmacokinetics   MeSH
• Small Molecule Libraries chemistry   pharmacokinetics   MeSH
• Humans MeSH
• Neoplasms pathology   radiotherapy   MeSH
• Drug Carriers administration & dosage   chemistry   MeSH
• Radiopharmaceuticals chemistry   therapeutic use   MeSH
• Radioisotopes chemistry   therapeutic use   MeSH
• Radium chemistry   therapeutic use   MeSH
• Dose-Response Relationship, Radiation MeSH
• Check Tag
• Humans MeSH
• Publication type
• Journal Article MeSH
• Review MeSH
• Names of Substances
• 1,4,7-triazacyclononane-N,N',N''-triacetic acid MeSH Browser
• 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid MeSH Browser
• Actinium-225 MeSH Browser
• Actinium MeSH
• Astatine MeSH
• Astatine-211 MeSH Browser
• Bismuth MeSH
• Bismuth-213 MeSH Browser
• Chelating Agents MeSH
• Heterocyclic Compounds, 1-Ring MeSH
• Heterocyclic Compounds MeSH
• Small Molecule Libraries MeSH
• Drug Carriers MeSH
• Radiopharmaceuticals MeSH
• Radioisotopes MeSH
• Radium-223 MeSH Browser
• Radium MeSH