Drug intelligence / Profile preview

astatobenguane [211At]

Development stage
Phase 1
Lead developer
Duke University
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Astatobenguane [211At] (also known as [211At]MABG) is an investigational alpha-emitting radiopharmaceutical designed for the targeted therapy of neuroendocrine tumors, including pheochromocytoma and paraganglioma. It is a structural analog of meta-iodobenzylguanidine (MIBG) and functions as a substrate for the norepinephrine transporter (NET), which is highly expressed on the surface of these tumor cells. Upon internalization, the Astatine-211 isotope undergoes alpha decay, releasing high-energy alpha particles with a short tissue range (50–80 µm). This localized radiation induces lethal double-strand DNA breaks in the tumor cells while sparing adjacent healthy tissue. Astatobenguane [211At] is being developed as a more potent alternative to [131I]MIBG, particularly for patients with metastatic or refractory disease, due to the higher relative biological effectiveness of alpha radiation compared to beta radiation.

Other names
astatine-211-labeled 3-astatobenzylguanidineastatine211-labeled 3-astatobenzylguanidineastatine 211-labeled 3-astatobenzylguanidinemeta-[211At]astatobenzylguanidine3-[211At]astatobenzylguanidine[211At]astatobenguane
02

Targets

NET (Norepinephrine Transporter)

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