⁶⁴Cu-Diasparagine (⁶⁴CuASP) is a ⁶⁴Cu-labeled peptide developed for the Imaging and treatment of glioblastoma.

Tumor cells need asparagine for cellular metabolic activities and ⁶⁴Cu is able to link DNA and to destroy tumor cells thanks to its Auger effect. In fact, the mechanism of action is characterized by high Linear Energy Transfer (LET) in a small spatial region that can crash the cell.

⁶⁴Cu-Diasparagine is able to cross the blood–brain barrier (BBB) and to link to cellular DNA. The drug has been tested in glioblastoma patients. Patient’s life expectancy has been extended up to 15 months after tumor diagnosis with enhanced quality of life. Doses of about 80 mCi have been used.

Only a few patients have been injected with ⁶⁴Cu-Diasparagine and the data generated so far are not sufficient to confirm the efficacy of this drug. This development is quite slow and probably due to the limited budget available.

Target/Mechanism: DNA

Carrier/Ligand: n/a

Radiation Type: C.E. (Conversion electron)