Advances in the sensitivity of detection by mass spectrometry have enabled its application to evaluate small molecule compounds as tracers in vivo without the need for radiolabelling the compound. The ability of a compound to differentially distribute toward target rich tissues in comparison to a tissue with no/less target present is the unique defining feature of a tracer. By microdosing non-labelled compounds in vivo and analyzing tissue levels by LC–MS/MS, compounds can be screened for their ability to function as tracers in a manner consistent with the target expression biology allowing for a more rapid iterative design cycle to find a PET tracer. This methodology can be further extended to preclinical receptor occupancy studies with a non-radiolabelled tracer to advance drug discovery and design of therapeutic molecules. Examples of PET tracer development and utility of preclinical receptor occupancy studies will be presented.

Application of LC-MS/MS techniques to the selection of PET tracers and determination of receptor occupancy in preclinical studies

251st National Meeting (2016)

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