AFLIBERCEPT IS A VEGF-TRAP MOLECULE BUILT FROM NATIVE RECEPTOR DOMAINS
Aflibercept is a fusion protein built from portions of the native human receptors VEGFR-1 and VEGFR-2. It acts as a decoy receptor for VEGF-A, VEGF-B, PlGF and Gal-1.
Aflibercept molecule
The rationale for testing a high molar dose
This is a purely illustrative hypothesis for duration of effect of a higher molar dose vs a lower molar dose. Preclinical and clinical testing of an agent must be conducted to determine the safety, efficacy and durability profiles.
Aflibercept’s VEGF suppression can be sustained for longer with EYLEA 8 mg vs EYLEA 2 mg
EYLEA 8 mg provides 4x the molar dose of aflibercept compared with EYLEA 2 mg, resulting in an effective concentration for longer in the eye.*
*Based on mathematical modelling and the clinical relevance is unknown.
Model of logarithmic intraocular drug concentration over time*
Adapted from Schubert W, et al. 2022 & EPAR report. 2024.
*The impact of molecular properties on clinical outcomes is yet to be defined. This is a hypothetical, illustrative model based on in vitro data.
PK models estimate that EYLEA 8 mg exhibits an unexpected 34% slower ocular clearance than EYLEA 2 mg
Slower ocular clearance facilitates longer VEGF suppression
Aflibercept’s long-lasting anti-VEGF activity is augmented by the higher molar dose of 8 mg vs 2 mg
Expert opinion on high molar dose with EYLEA 8 mg
Michael Stewart, Professor of Ophthalmology Research (Mayo Clinic, Florida), talks about the rationale behind the high molar dose and pharmacokinetics of EYLEA 8 mg.
Prescribing information for EYLEA® (aflibercept) can be found here.
Abbreviations
DMO, diabetic macular oedema. Fc, fragment crystallisable. Gal-1, galectin-1. IgG, immunoglobulin G. nAMD, neovascular (wet) age-related macular degeneration. PK, pharmacokinetic. PIGF, placental growth factor. VEGF, vascular endothelial growth factor. VEGFR, vascular endothelial growth factor receptor.
PP-EYL-GB-2794 | March 2025