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Microdosing Studies in Humans

The Role of Positron Emission Tomography

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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.

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Acknowledgements

No sources of funding were used to assist in the preparation of this review. The authors have no conflicts of interest that are directly relevant to the content of this review.

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Authors and Affiliations

  1. Department of Clinical Pharmacology, Medical University Vienna, Währinger-Gü rtel 18–20, Vienna, 1090, Austria

    Martin Bauer, Claudia Christina Wagner &  Oliver Langer

  2. Department of Radiopharmaceuticals, Austrian Research Centers GmbH-ARC, Seibersdorf, Austria

    Oliver Langer

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  1. Martin Bauer
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  2. Claudia Christina Wagner
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  3. Oliver Langer
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Correspondence to Oliver Langer.

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Bauer, M., Wagner, C.C. & Langer, O. Microdosing Studies in Humans. Drugs R&D 9, 73–81 (2008). https://doi.org/10.2165/00126839-200809020-00002

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