68Ga-Labeled Compounds for PET Myocardial Perfusion Imaging

2016 Fiscal Year Final Research Report

• Project/Area Number: 15H06097
• Research Category: Grant-in-Aid for Research Activity Start-up
• Allocation Type: Single-year Grants
• Research Field: Radiation science
• Research Institution: Chiba University
• Principal Investigator: Mahmood Ashfaq 千葉大学, 大学院薬学研究院, 特任教授 (30754775)
• Project Period (FY): 2015-08-28 – 2017-03-31
• Keywords: PET / gallium / heart

Outline of Final Research Achievements

An important clinical PET application is in myocardial perfusion imaging (MPI) for heart disease. The aim of this research was to synthesize and evaluate new 67/68Ga-complexes for PET MPI.
We studied two separate classes of new hexadentate chelates (N4S2 and N4O2) that can easily be modified with substituents, provide stable complexation of Ga(III), and result in lipophilic, monocationic [Ga-complexes]+, properties necessary for myocardial uptake. Ligands for both chelate classes were synthesized and their Ga-complexes provided mono-cationic Ga-complexes. Radiolabeling with 67Ga(III) achieved high radiochemical yield in 30 min. In-vivo studies in normal mice display in-vivo stability, rapid distribution and clearance with low myocardial uptake due to lower lipophilicity compared to 99mTc-MIBI. Further modifications for increased lipophilicity and improved myocardial retention are required to attain a effective PET myocardial perfusion agent with high myocardial uptake.

Free Research Field

Radiopharmaceutical chemistry