Fluorine-18 labeled synthetic alicyclic amino acids, are a class of a,a-dialkyl amino acids with side chains that are covalently bonded to each other to form a cyclic ring and are a diverse and useful class tumor imaging agents suitable for positron emission tomography (PET). These tracers target the increased expression of cell membrane amino acid transporters exhibited by many human tumor cells. The most established clinical use for radiolabeled amino acids is imaging primary and recurrent gliomas, and primary, recurrent and metastatic and prostate cancer. This presentation focuses on the synthesis, radiolabeling, preclinical and clinical evaluation of a series of non-natural fluorine-18 labeled amino acids: 1-amino anti/syn-3-fluorocyclobutane-1-carboxylic acid, enantiomerically enriched 1-amino anti-2-fluorocyclobutane-1-carboxylic acid and 1-amino anti-2-fluorocyclopetane-1-carboxylic acid. Research supported by NIH, Georgia Cancer Coalition, Georgia Research Alliance and Nihon Mediphysics Japan. The radiotracers reported in this presentation are either eligible for royalties to Emory University and Mark M. Goodman.

Fluorine-18 synthetic amino acids as PET tumor imaging agents

243rd National Meeting (2012)

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