Physiologically Based Pharmacokinetic (PBPK) Modeling to Predict PET Image Quality of Three Generations EGFR TKI in Advanced-Stage NSCLC Patients.

ABSTRACT:

Introduction

Epidermal growth factor receptor (EGFR) mutated NSCLC is best treated using an EGFR tyrosine kinase inhibitor (TKI). The presence and accessibility of EGFR overexpression and mutation in NSCLC can be determined using radiolabeled EGFR TKI PET/CT. However, recent research has shown a significant difference between image qualities (i.e., tumor-to-lung contrast) in three generation EGFR TKIs: ¹¹C-erlotinib, ¹⁸F-afatinib and ¹¹C-osimertinib. In this research we aim to develop a physiological pharmacokinetic (PBPK)-model to predict tumor-to-lung contrast and as a secondary outcome the uptake of healthy tissue of the three tracers.

Methods

Relevant physicochemical and drug specific properties (e.g., pKa, lipophilicity, target binding)

SUBMITTER: Bartelink IH 

PROVIDER: S-EPMC9315544 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature