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Microdosing Studies in Humans

Martin Bauer, Cláudia Wagner, Oliver Langer

Drugs in R&D 2008 DOI: 10.2165/00126839-200809020-00002 (opens in new tab)

Study at a glance

AI-extracted from the abstract
Characteristics Review Peer reviewed
Topics Microdosing
Keywords Pharmacology
Citations 52
Key findings PET-microdosing can describe a drug's concentration-time profile in body tissues with minimal toxicological risk and reduced preclinical safety testing, potentially shortening drug development timelines and cutting costs.

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.