Exploring the Potential of Astatine-211 in Oncology

Astatine-211 for Targeted Alpha Radiotherapy and Drug Development

Synonyms: Astatine-211, ²¹¹At, At-211, alpha emitter, targeted alpha therapy (TAT), alpha radiotherapy, radiolabeled small molecules, radiolabeled peptides, radiopharmaceutical research, alpha particle isotope, radioligand therapy

Astatine-211 (²¹¹At) is an alpha-emitting radioisotope with unique potential in targeted alpha therapy (TAT) for cancer and other diseases requiring high-precision cytotoxicity. Its short-range, high-linear energy transfer (LET) alpha particles enable the selective destruction of malignant cells while minimizing damage to surrounding healthy tissue. In preclinical and translational research, ²¹¹At is often conjugated to small molecules, peptides, or other targeting vectors to evaluate therapeutic efficacy and dosimetry in novel drug candidates.

Astatine-211 (²¹¹At) Details:

Radiation Type: Alpha emitter (energy ~5.87 MeV)
Half-life: ~7.2 hours – suitable for targeted delivery and rapid clearance

Primary Applications:

• Targeted alpha therapy for hematologic malignancies and solid tumors
• Radiolabeling of small molecules and peptides
• Preclinical pharmacokinetics, biodistribution, and efficacy studies

Benefits in Drug Discovery:

• High-LET radiation for potent tumor cell killing
• Short path length (~70 µm) reduces off-target toxicity
• Versatility in conjugation chemistry for diverse targeting agents
• Suitable for both early-stage preclinical validation and translational studies
• Potential for theranostic pairing with iodine isotopes for imaging

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