Astatine-211 and actinium-225: two promising nuclides in targeted alpha therapy

• Targeted alpha therapy (TAT) using 211At and 225Ac offers high-energy, short-range α-particles that cause irreparable DNA damage, effectively killing tumor cells while sparing surrounding healthy tissue. • 211At- and 225Ac-labeled radiopharmaceuticals show promising results in preclinical and clinical trials for targeting PSMA in prostate cancer, CD in hematological malignancies, HER2 in ovarian cancer, and SSTR in neuroendocrine tumors. • The unique physicochemical properties of 211At and 225Ac, including suitable half-lives and minimal toxic decay products, make them ideal candidates for advancing TAT in clinical practice. • Ongoing research focuses on optimizing chelation chemistry and targeting vectors to enhance the efficacy and safety of 211At-/225Ac-based therapies, potentially expanding their application to a wider range of cancers.