Snythesis of [F-18]-ZD1839 as a PET Imaging Agent for Epidermal Growth Factor Receptors
Physics and Astronomy
The epidermal growth factor receptor (EGFR) is an epithelial cell membrane receptor with an intra- cellular tyrosine kinase (TK) component. EGFR-TK is involved in cell signalling critical to proliferation, apoptosis, repair and angiogenesis. More than two thirds of human cancers derive from epithelial tissues and the EFGR-TK is overexpressed in the majority of these tumors. Thus in recent years numerous selective EGFR-TK inhibitors with nanomolar affinities have been developed as potential anti-cancer agents. One potent inhibitor that has progressed the furthest toward clinical registration is ZD1839 (or Iressa). ZD1839 is approved for clinical use in Japan and is close to obtaining U.S. FDA approva l. ZD1839 is a fluorine-containing anilinoquinazoline which can be isotopically labelled with 18F for use in clinical oncology as a PET imaging agent. Since extensive pre-clinical and clinical data on ZD1839 are available, the use of 18F-ZD1839 to identify patients who would benefit from Iressa treatment and monitor its efficacy would be straightforward.
Abstract from the 15th International Symposium on Radiopharmaceutical Chemistry - Session 1: Oncology: Molecular Markers and Tumour Diagnosis I - Chemistry and Pharmacology.
Journal of Labelled Compounds and Radiopharmaceuticals
O.T. DeJesus, D. Murali, L.G. Flores, A.K. Converse, D.W. Dick, T.R. Oakes, A.D. Roberts, and R.J. Nickles. (2003). Synthesis of [F-18]-ZD1839 as a PET Imaging Agent for Epidermal Growth Factor Receptors. Journal of Labelled Compounds and Radiopharmaceuticals, 46(S1), S1-S9.
Publisher's Copyright and Source
Copyright © 2003 John Wiley & Sons. Article published by John Wiley & Sons in Journal of Labelled Compounds and Radiopharmaceuticals, volume 46, supplement 1, August 2003, pages S1-S9. Available online on August 7, 2003: http://doi.org/10.1002/jlcr.750.