Preclinical to Clinical Translation of Pharmacokinetic-Pharmacodynamic Relationship in EGFR Exon20Ins Mutations: A Modeling Framework for Irreversible Inhibitors.

doi:10.1158/1535-7163.MCT-25-0082

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Preclinical to Clinical Translation of Pharmacokinetic-Pharmacodynamic Relationship in EGFR Exon20Ins Mutations: A Modeling Framework for Irreversible Inhibitors.

Molecular cancer therapeutics - 2 Jul 2026

Savoca Adriana, Zindel Diana, Polanski Radoslaw, Kostomiris Demetrios H, Pirmoradian Mohammad, Swaih Aisha M, Talbot Sara, Floc'h Nicolas, Winlow Poppy, Davey Paul R J, Longmire David, Wadforth Emma, Lewis Hilary J, Smith Aaron, Lipka Rebecca, Wilson Joanne, Britton David James, Dokal Arran D, Smith Ryan, Thomson Clare, McCoull William

Abstract excerpt

Epidermal growth factor receptor (EGFR) Exon20 insertions (Exon20Ins) constitute the third most common EGFR activating mutation in non-small cell lung cancer. We developed a semimechanistic pharmacodynamic model for irreversible inhibitors of EGFR Exon20Ins mutations by integrating kinetic data of proprietary compounds with a mechanistic description of EGFR turnover and phosphorylation to investigate the...

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PMID: 41622600
DOI: 10.1158/1535-7163.MCT-25-0082

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