lead-212

Lead-212 is a radioactive isotope of lead used as a source of alpha radiation in targeted cancer therapies, especially in the emerging field of targeted alpha therapy (TAT). With a half-life of approximately 10.64 hours, lead-212 decays by beta emission to bismuth-212, which further decays to provide potent alpha emission. In drug development, lead-212 is commonly chelated to targeting molecules (e.g., somatostatin analogues, monoclonal antibodies) via agents like DOTA, DOTAM, or TCMC to form radiopharmaceutical conjugates. These agents selectively bind tumor antigens or receptors, delivering cytotoxic alpha radiation precisely to cancer cells while minimizing harm to healthy tissue. Lead-212’s high linear energy transfer and short particle path dramatically increase DNA double-strand breaks in malignant cells, offering a particularly effective therapy for tumors resistant to conventional beta-emitting radiotherapies. Lead-212-based therapies are being evaluated for various solid tumors (notably neuroendocrine tumors) and hematologic malignancies[1][2][3]. Its principal use is as the radioisotope payload of radiopharmaceutical drugs, rather than as a stand-alone drug or product.

Other names

212PbPb-212Pb212Pb 212radioactive lead-212^212Pb