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211At-iso-GMAB-PEG3-TOC
- Development stage
- Preclinical
- Lead developer
- Korea Institute of Radiological and Medical Sciences
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
211At-iso-GMAB-PEG3-TOC is a targeted alpha therapy (TAT) radiopharmaceutical being developed by the Korea Institute of Radiological and Medical Sciences (KIRAMS) for the treatment of somatostatin receptor (SSTR)-expressing neuroendocrine tumors. The compound consists of the alpha-emitting radionuclide astatine-211 (211At) conjugated to the somatostatin analog [Tyr3]octreotide (TOC) via an iso-GMAB prosthetic group and a PEG3 linker. The iso-GMAB prosthetic group and PEG3 linker are designed to improve the in vivo stability and biodistribution of the 211At-labeled compound, while TOC provides high-affinity targeting to SSTRs. In preclinical studies, 211At-iso-GMAB-PEG3-TOC demonstrated dose-dependent tumor growth suppression and significant survival extension in SSTR-expressing AR42J tumor-bearing mice without causing severe systemic toxicity.
02
Targets
SSTR2 (Somatostatin receptor type 2)
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