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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.
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
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
- Referencesexpand_less
- 1EYLEA® 114.3 mg/mL Summary of Product Characteristics.
- 2Papadopoulos N, et al. Angiogenesis 2012;15:171–185.
- 3Kanda A, et al. Sci Rep 2015;5:17946.
- 4Schubert W, et al. Transl Vis Sci Technol 2022;11:36.
- 5Assessment report. Aflibercept. Accessed: August 2024.
- 6Veritti D, et al. Pharmaceutics 2023;15:1416.