Microdosing in early lead discovery.
A P Jekunen, E K J Pauwels, K J A Kairemo
Bioanalysis March 2010 DOI: 10.4155/bio.09.189 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Topics | Microdosing |
| Key findings | Argues that microdosing can enhance drug development by enabling early human studies, supporting go/no-go decisions and lead selection, and providing biodistribution data, with time and cost savings, though its real value is not yet established due to limited published reports. |
Abstract
Microdosing provides a tool to enhance drug development by initiating human studies prior to Phase I studies. The purpose is to assist in the go versus no-go decision-making process and to eliminate early ineffective compounds from the drug pipeline. Selection of multiple potential leads can be performed at the clinical stage instead of in preclinical studies. The microdosing approach can be easily used for a molecularly targeted potential drug compound with a known mechanism of action. It provides useful data regarding accessibility and biodistribution that can be used in many estimations benefiting the development of the molecule. In addition, steady state and genetic investigations are becoming possible. Microdosing has a sparing effect on timelines and costs, however, the real importance is not yet known because, although it is known to be widely performed, only a few original reports have been published.