Evaluation of [¹⁸F]AlF-EMP-105 for Molecular Imaging of C-Met

• Main Authors: Jin Hui Teh (Author), Ala Amgheib (Author), Ruisi Fu (Author), Chris Barnes (Author), Joel Abrahams (Author), Ali Ashek (Author), Ning Wang (Author), Zixuan Yang (Author), Muneera Mansoorudeen (Author), Nicholas J. Long (Author), Eric O. Aboagye (Author)
• Format: Book
• Published: MDPI AG, 2023-07-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

C-Met is a receptor tyrosine kinase that is overexpressed in a range of different cancer types, and has been identified as a potential biomarker for cancer imaging and therapy. Previously, a ⁶⁸Ga-labelled peptide, [⁶⁸Ga]Ga-EMP-100, has shown promise for imaging c-Met in renal cell carcinoma in humans. Herein, we report the synthesis and preliminary biological evaluation of an [¹⁸F]AlF-labelled analogue, [¹⁸F]AlF-EMP-105, for c-Met imaging by positron emission tomography. EMP-105 was radiolabelled using the aluminium-[¹⁸F]fluoride method with 46 ± 2% RCY and >95% RCP in 35-40 min. In vitro evaluation showed that [¹⁸F]AlF-EMP-105 has a high specificity for c-Met-expressing cells. Radioactive metabolite analysis at 5 and 30 min post-injection revealed that [¹⁸F]AlF-EMP-105 has good blood stability, but undergoes transformation-transchelation, defluorination or demetallation-in the liver and kidneys. PET imaging in non-tumour-bearing mice showed high radioactive accumulation in the kidneys, bladder and urine, demonstrating that the tracer is cleared predominantly as [¹⁸F]fluoride by the renal system. With its high specificity for c-Met expressing cells, [¹⁸F]AlF-EMP-105 shows promise as a potential diagnostic tool for imaging cancer.

Item Description

10.3390/pharmaceutics15071915
1999-4923