Title: Automated preparation of [18F]-MG11, using [18F] F-Py-TFP, [18F] SFB and [18F] NFP radiosynthons, through iPHASE FlexLab radiosynthesis platform, for PET imaging of cancer

Biography:

Naeem-Ul-Haq Khan has recently submitted his PhD dissertation at Govt. College University, Faisalabad-Pakistan and performed his research work at University of Melbourne, and Peter MacCallum Cancer Centre, Melbourne, Australia. He worked as a research associate at Pakistan Institute of Nuclear Science and Technology, Islamabad-Pakistan. He has published more than 6 papers in good impacted journals and presented his research work in more than 12 national and international conferences.

Abstract

For diagnosis of malignancies and other disease conditions, [¹⁸F] FDG and to lesser extent the other small molecules have become important clinical radio tracers. In USP, only three [¹⁸F]-radiopharmaceuticals [¹⁸F] FDG, [¹⁸F] fluorodopa and [¹⁸F] NaF have been listed for PET imaging. [¹⁸F]-labeled peptides have also been developed as promising target specific imaging agents. In this study, cold standard FPro-MG11, FBen-MG11 and FPy-MG11 have been synthesized using solid phase peptide synthesis technique. The three [¹⁸F]-radiosynthons, [¹⁸F] F-Py-TFP, [¹⁸F] SFB and [¹⁸F] NFP  have been synthesized through TRACER Lab FX-FN module to radiolabel the model peptide MG11 through its N-terminus and investigate the biological effect of resulting radiotracers. The iPHASE FlexLab module was used to radiolabel MG11 peptide by using these radiosynthons [¹⁸F] F-Py-TFP, [¹⁸F] SFB and [¹⁸F] NFP. Automated peptide radiolabeling experiments for [¹⁸F] FNic-MG11 synthesis provided more radiolabeling yield and specific activity than for other two analogs [¹⁸F] FB-MG11 and [¹⁸F] FP-MG11. Further, all these [¹⁸F]-prosthetic groups radiolabeled the peptide in site selective manner. Scintigraphy results provides T/NT ratio 7.02 ± 0.98 which is more than other two and found consistent with biodistribution data. Radioactive experiments like scintigraphy, biodistribution, blocking studies, internalization study, autoradiography and H & E staining study and non-radioactive experiments like ligand binding study, hydrophilicity study demonstrated that all the three analogues of MG11 peptide reacted in a target specific manner and proved suitable for PET imaging of CCK-2 receptor positive cancer.