Fluorine-18 labelling of a series of potential EGFRvIII targeting peptides with a parallel labelling approach using [18F]FPyME

There is growing interest in the use of radiolabelled peptides as receptor targeting agents for diagnostic imaging of various cancer types using positron emission tomography. In this work, 1-[3-(2-[ 18 F]fluoropyridin-3-yloxy)propyl]pyrrole-2,5-dione ([ 18 F]FPyME) has been used for parallel fluorine-18 labelling of PEPHC1, a peptide selective towards the cancer-specific mutation of the epidermal growth factor receptor (EGFRvIII), and a number of truncated and mutated analogues. Conjugation of the peptides with [ 18 F]FPyME was achieved within 10 min in non-decay-corrected radiochemical yields of 30–50%. The high yield of the conjugation reaction combined with its short synthesis time allows the labelling of several peptides from a single batch of [ 18 F]FPyME.