Microdosing studies using accelerated mass spectrometry as exploratory investigational new drug trials

Microdosing studies, which use subpharmacological doses of drug candidates, offer early information on how the body processes these compounds, potentially reducing costs and improving productivity in early clinical drug development. Highly sensitive analytical technology, particularly accelerator mass spectrometry (AMS), enables qualitative and quantitative assays of labeled compounds in humans, providing pharmacokinetic and metabolic data for candidate selection. The applicability of microdosing is expanding into absolute bioavailability and mass balance studies. It remains uncertain whether microdosing adequately predicts therapeutic-dose pharmacokinetics, but further development of AMS-based microdosing may benefit drug development and pose new challenges for researchers. Introducing this method in Korea could enhance competitiveness in pharmaceutical research and development.

Study at a glance

Abstract

Innovative attempts have been made to overcome nonproductivity and high expenditure in the clinical stages of new drug development. Microdosing studies using subpharmacological doses provide early insight into the body's disposition toward candidate compounds, and are innovative exploratory trials that can promote productivity in drug development. Highly sensitive analytical technology is crucial in microdosing studies that employ qualitative and quantitative assays of target materials in humans. Accelerator mass spectrometry (AMS) has facilitated the adoption of a human microdosing study in the early phase of clinical drug development. Results derived from AMS microdosing studies using labeled compounds can provide various types of information for candidate selection, including pharmacokinetic characteristics and metabolic profiles of candidate compounds. The applicability of microdosing studies is currently expanding into absolute bioavailability and mass balance studies. Although it remains uncertain whether microdosing adequately predicts the pharmacokinetics of therapeutic doses, further development of microdosing studies using AMS may benefit the field of new drug development and could pose a new challenge to researchers. The use of advanced technology in candidate selection will contribute to improved productivity and competitiveness in pharmaceutical research and development. The introduction of microdosing studies using AMS in Korea will present a newly applicable method for innovative clinical trials and contribute to development potential in global competition.