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Phase 0/microdosing approaches: time for mainstream application in drug development?

Tal Burt, Graeme Young, Wooin Lee, Hiroyuki Kusuhara, Oliver Langer, Malcolm Rowland, Yuichi Sugiyama

Nature Reviews Drug Discovery September 8, 2020 DOI: 10.1038/s41573-020-0080-x (opens in new tab)

Study at a glance

AI-extracted from the abstract
Characteristics Review Peer reviewed
Topics Microdosing
Keywords Mainstream Drug development Pharmacology
Citations 101
Key findings Phase 0 approaches can improve preclinical candidate selection and enable safer, cheaper, quicker, and more informed developmental decisions.

Abstract

Phase 0 approaches - which include microdosing - evaluate subtherapeutic exposures of new drugs in first-in-human studies known as exploratory clinical trials. Recent progress extends phase 0 benefits beyond assessment of pharmacokinetics to include understanding of mechanism of action and pharmacodynamics. Phase 0 approaches have the potential to improve preclinical candidate selection and enable safer, cheaper, quicker and more informed developmental decisions. Here, we discuss phase 0 methods and applications, highlight their advantages over traditional strategies and address concerns related to extrapolation and developmental timelines. Although challenges remain, we propose that phase 0 approaches be at least considered for application in most drug development scenarios.