Drug intelligence / Profile preview

[64Cu]Cu-DOTA-(PEG28)2-A20FMDV2

Development stage
Preclinical
Lead developer
Washington University School of Medicine
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration
Intravenous
01

Overview

[64Cu]Cu-DOTA-(PEG28)2-A20FMDV2 is a radiopharmaceutical imaging agent designed for positron emission tomography (PET). It consists of the A20FMDV2 peptide, a 20-amino-acid sequence derived from the foot-and-mouth disease virus that specifically binds to the integrin αvβ6 receptor. To optimize its pharmacokinetic profile, the peptide is bi-terminally PEGylated with two PEG28 chains and conjugated to a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) chelator for radiolabeling with the positron-emitting isotope Copper-64 (64Cu). Integrin αvβ6 is an epithelial-specific receptor that is significantly upregulated in various aggressive malignancies, including pancreatic, cervical, and non-small cell lung cancers, while remaining largely absent in normal adult tissues. This makes the drug a highly specific probe for detecting primary tumors and metastatic lesions. The bi-terminal PEGylation strategy is employed to reduce rapid excretion and metabolic breakdown, thereby enhancing tumor uptake and retention compared to non-PEGylated or mono-PEGylated versions.

Other names
64Cu-DOTA-(PEG28)2-A20FMDV2Copper-64 DOTA-bi-PEGylated A20FMDV2Copper64 DOTA-bi-PEGylated A20FMDV2Copper 64 DOTA-bi-PEGylated A20FMDV2
02

Targets

αVβ6 (Integrin αVβ6)

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