The effect of ligand amount, affinity and internalization on PSMA-targeted imaging and therapy: A simulation study using a PBPK model.

ABSTRACT: The aim of this work was to investigate the effect of ligand amount, affinity and internalization of prostate-specific membrane antigen (PSMA)-specific ligands on the activity concentrations for PET/CT imaging and on the absorbed doses for therapy. A physiologically-based pharmacokinetic (PBPK) model for PSMA-specific ligands was implemented. Thirteen virtual patients with metastatic castration-resistant prostate cancer were analysed. Simulations were performed for different combinations of association rates k_on (0.1-0.01 L/nmol/min), dissociation rates k_off (0.1-0.0001 min^-1), internalization rates λ_int (0.01-0.0001 min^-1) and ligand amounts (1-1000 nmol). For imaging the activity was normalized to volume and injected activity (⁶

SUBMITTER: Begum NJ 

PROVIDER: S-EPMC6934468 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature