Drug intelligence / Profile preview

[211At]3'-At-PIB-OH

Development stage
Preclinical
Lead developer
University of Utah
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Alpha Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

`[211At]3'-At-PIB-OH` is a preclinical small-molecule radiopharmaceutical designed for targeted alpha therapy (TAT) of Alzheimer's disease. It is an astatinated derivative of the Pittsburgh compound B (PIB) scaffold, specifically developed as an alpha-emitting analog of the FDA-approved PET imaging agent Vizamyl (flutemetamol). The compound consists of a benzothiazole scaffold radiolabeled with astatine-211 ($^{211}\text{At}$), a 7.2-hour half-life alpha emitter. It is designed to cross the blood-brain barrier and selectively target amyloid-beta ($\text{A}\beta$) aggregates (amyloid plaques) in the brain, delivering localized high-energy alpha radiation to disrupt the plaques and potentially stimulate a protective immune response. Preclinical studies in mouse models of Alzheimer's disease have demonstrated that the compound crosses the blood-brain barrier, is well-tolerated, and significantly reduces amyloid-beta plaque concentrations. The compound is being developed by researchers at the University of Utah and the University of Washington.

Other names
211At-3'-At-PIB-OHastatinated PIB-OHastatinated version of Vizamyl
02

Targets

Aβ (Amyloid-beta peptides and aggregates)

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