Evaluation of Molecular Properties versus In Vivo Performance of Aflibercept, Brolucizumab, and Ranibizumab in a Retinal Vascular Hyperpermeability Model.

ABSTRACT:

Purpose

To evaluate the molecular, pharmacokinetic, and pharmacological properties of three anti-vascular endothelial growth factor (VEGF) agents-aflibercept, brolucizumab, and ranibizumab-and to provide a prediction of the optimal design of an intravitreal VEGF challenge in rabbits to assess the preclinical in vivo activity of the different anti-VEGF agents.

Methods

Biochemical analyses and cellular and animal models of retinopathy were used to characterize anti-VEGF efficacy. Anti-VEGF biochemical binding affinity was determined through a kinetic exclusion assay. The in vitro potency was investigated by a calcium mobilization assay. Pharmacokinetic parameters were estimated for each drug to predict intraocular exposure relationships among the agents. The in silico modeling

SUBMITTER: Schubert W 

PROVIDER: S-EPMC9617509 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature