A phase 0 clinical trial of novel candidate extended-release formulations of capecitabine

Abstract

Modulation of capecitabine release in patients can be accomplished by varying tablet coating content. Proof of principle was demonstrated for candidate ER formulations with coating content of 3 mg/cm(2).

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

“…Multiple preclinical candidates 11,12,97,[100][101][102][103][104]133 Selection using cassette microdosing 11 Microdosing study results and PBPK modelling combined to inform candidate selection 104 Conflicting or inadequate preclinical data Uncertainty in extrapolating pharmacokinetic and/or pharmacodynamic data from preclinical models to humans…”

“…This application has been used in novel drug development (Table 3) and is most appropriate when the candidates are not sufficiently differentiable on the basis of preclinical data alone 11,12,97,[100][101][102][103][104]133 . The first such application used microdoses of three preclinical analogues and therapeutic doses of two structurally similar H 1 antagonist analogues, administered orally and intravenously, to characterize pharmacokinetic profiles where preclinical data were unable to separate the candidates 97 .…”