Automated Synthesis Module for Labeling Peptides with Fluorine-18

78763S 18F-FDG ([18F]2-deoxy-2-fluoro-D-glucose) is widely used for the diagnosis, staging, and monitoring of malignancies using positron emission tomography (PET). However, its accumulation in tissue is not specific to malignancies only, and also is ineffective for detecting cancers with no enhanced glucose utilization. Consequently, there is a great need to develop tumor-selective PET agents. Both higher target-to-background ratios and rapid blood clearance can often be achieved by using receptor-avid peptides as targeting vectors, due to their smaller size and high binding affinities. Unfortunately, the 18F-labeled peptides are not suitable for clinical use due to their laborious (multi-step synthesis and purification required) labeling methods, currently performed manually in sophisticated laboratories by highly trained personnel. This project will develop and an automated synthesis module for easy and efficient preparation of the 18F-labeled peptide-based PET radiopharmaceuticals routinely. Phase I will: (1) optimize system design in preliminary studies to avoid potential problems and to address safety issues, (2) develop a first generation prototype design based on the optimized system design, and (3) fabricate and test the first generation prototype using a non-radioactive surrogate. Commercial Applications and Other Benefits as described by the awardee: Positron emission tomography (PET) is currently the fastest growing segment of nuclear medicine due to its superior sensitivity, spatial resolution, and quantification. Growth should continue with procedure volume increasing about 35%, reaching 2.1 million procedures by 2010. New PET imaging probes should expand the range of classical indications that can use PET as a diagnostic tool and also increase the economical benefits to PET centers.