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64Cu-NOTA-cysVar3
- Development stage
- Preclinical
- Lead developer
- Memorial Sloan Kettering Cancer Center
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
- Administration
- Intravenous
01
Overview
64Cu-NOTA-cysVar3 is a radiopharmaceutical diagnostic agent designed for positron emission tomography (PET) imaging of the acidic tumor microenvironment. It consists of the radionuclide copper-64 (64Cu) chelated by 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA), which is conjugated to a cysteine-containing variant of the pH (low) insertion peptide (pHLIP), specifically Var3. The pHLIP technology exploits the characteristic extracellular acidity of tumors; at low pH, the peptide undergoes a conformational change that triggers its insertion into the cell membrane, effectively delivering the imaging isotope to the cancer site. This mechanism allows for targeting of various metabolic tumors regardless of specific receptor expression. Preclinical studies have demonstrated its efficacy in imaging breast, prostate, and melanoma models.
- Other names
- 64Cu-NOTA-pHLIP Var364Cu-NOTA-cys-pHLIP Var3
02
Targets
Cellular lipid bilayer in low extracellular pH
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