Drug intelligence / Profile preview

[225Ac]ac-dota-trastuzumab fab

Development stage
Preclinical
Lead developer
University of Toronto
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Antibody Fragments → Engineered Antibody Formats → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[225Ac]ac-dota-trastuzumab fab is a preclinical-stage targeted alpha-particle radioimmunotherapy (TART) agent. It consists of the antigen-binding fragment (Fab) of the anti-HER2 monoclonal antibody trastuzumab, conjugated to the chelator DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) and radiolabeled with the alpha-particle-emitting radionuclide actinium-225 ([225Ac]). The agent is designed to target human epidermal growth factor receptor 2 (HER2)-positive cancers, such as HER2-positive breast cancer. By utilizing a Fab fragment instead of a full-length IgG antibody, the agent exhibits faster blood clearance and reduced hematological toxicity, although it has higher renal uptake. It was developed by researchers at the University of Toronto.

Other names
225Ac-DOTA-trastuzumab Fab[225Ac]Ac-DOTA-trastuzumab Fabactinium-225 DOTA-trastuzumab Fabactinium225 DOTA-trastuzumab Fabactinium 225 DOTA-trastuzumab Fabactinium-225-labeled DOTA-trastuzumab Fabactinium225-labeled DOTA-trastuzumab Fabactinium 225-labeled DOTA-trastuzumab Fab
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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