Drug intelligence / Profile preview

bismuth-213

Development stage
Unknown
Lead developer
The University of New Mexico
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Bismuth-213 is a radioactive isotope and a potent alpha-emitting radionuclide used primarily in targeted alpha therapy (TAT) for cancer treatment. With a half-life of approximately 45.6 minutes, it emits high linear energy transfer (LET) alpha particles, enabling highly localized delivery of cytotoxic radiation to cancer cells while minimizing collateral damage to surrounding healthy tissue. Bismuth-213 is not used alone but is conjugated to targeting vectors, such as monoclonal antibodies or peptides (e.g., DOTATOC, HuM195), that bind specific tumor antigens or receptors. Upon binding, it delivers lethal, irreparable double-stranded DNA breaks to the tumor cells. Its main parent isotope is actinium-225, from which it is derived via a generator system. Bismuth-213-labeled radiopharmaceuticals are in preclinical and clinical use for diverse malignancies, including leukemia, lymphoma, neuroendocrine tumors, glioma, melanoma, bladder cancer, and brain tumors. Bismuth-213 is considered a "magic bullet" in targeted radionuclide therapy due to its high efficacy in cell killing, especially in patients resistant to beta-emitter therapies.[1][2][3][4][5][7][8]

Other names
213BiBi-213Bi213Bi 213Bismuth 213Bismuth213Bismuth-213
02

Targets

DNA

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