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Updated: Jun 26, 2026

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
Published on: April 3, 2026
Early integration of pharmacokinetic and dynamic reasoning is essential for optimal development of lead compounds:
Johan Gabrielsson1, Hugues Dolgos, Per-Göran Gillberg
1Discovery DMPK & BAC CVGI, AstraZeneca R&D Mölndal, S-431 83 Mölndal, Sweden. Johan.Gabrielsson@Astrazeneca.com
Abstract:
The aims of this report are firstly to raise awareness among kineticists and pharmacologists as to why pharmacokinetic-pharmacodynamic (PKPD) integration is essential for target validation (TV), optimizing development of lead compounds (lead generation [LG] and lead optimization [LO]) and scaling these to human. A related aim is to demonstrate strategic examples of PKPD collaborations that have improved the planning, execution and evaluation of experiments in primary and safety pharmacology. Examples include design of TV studies, design and data 'pruning' of PKPD studies in LO, analysis of data with marginal and substantial temporal (time) differences between exposure and response, design of safety pharmacology studies, assessment of safety margin and assessment of uncertainties in predictions of first dose in human.
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