Microdosing Studies in Humans

Positron emission tomography (PET)-microdosing involves giving human subjects a carbon-11- or fluorine-18-labeled drug candidate in microgram amounts to track the drug's concentration over time in targeted body tissues. Because only tiny amounts of unlabeled drug are used, toxicological risk is very low, and regulatory authorities require less preclinical safety testing than for conventional phase 1 studies. Microdose studies are becoming more important in clinical drug research because they can shorten development timelines and reduce costs. The review covers current PET applications in anticancer, anti-infective, and central nervous system drug research.

Study at a glance

Abstract

Positron emission tomography (PET)-microdosing comprises the administration of a carbon-11- or fluorine-18-labelled drug candidate to human subjects in order to describe the drug's concentration-time profile in body tissues targeted for treatment. As PET microdosing involves the administration of only microgram amounts of unlabelled drug, the potential toxicological risk to human subjects is very limited. Consequently, regulatory authorities require reduced preclinical safety testing as compared with conventional phase 1 studies. Microdose studies are gaining increasing importance in clinical drug research as they have the potential to shorten time-lines and cut costs along the critical path of drug development. Current applications of PET in anticancer, anti-infective and CNS system drug research are reviewed.