The Use of Microdosing in the Development of Small Organic and Protein Therapeutics
Journal of Nuclear Medicine May 25, 2017 Mats Bergström 31 citations
Microdosing uses very low, radionuclide-labeled drug doses for early human imaging or pharmacokinetic studies, requiring only a reduced preclinical toxicology package to lower cost and speed development. The approach limits exposure and risk by testing small populations for short periods. However, extrapolating results to therapeutic doses demands special attention to low-dose behavior, especially for small organic molecules versus protein therapeutics. The article reviews these aspects and discusses microdosing's role in drug development according to three pillars: tissue distribution and target access, target engagement, and induction of relevant tissue responses.