Aflibercept (Eylea) Biosimilars Pipeline Review

Aflibercept (Eylea) Biosimilars Pipeline Review

Reference Product: Eylea

Target: Vascular endothelial growth factor A (VEGF-A) & placental growth factor (PLGF)

Product Categories: Antibodies

This product provides basic information on approved drugs and drug candidates in research and development as biosimilar antibodies of Eylea (aflibercept).

This product consists of:

• Competitors described in a tabular format covering drug code/INN, target(s)/MoA, class of compound, territory of main competitor, indication(s) & R&D stage.
• Project History with link to source of information (press release, homepage, abstracts, presentations, annual reports etc).
• One-month online access to La Merie Publishing’s database for aflibercept (Eylea) biosimilars (prerequisite: access to internet).

This product is delivered on the very same day by e-mail containing competitor and project history reports in pdf format and database credentials. Reports are prepared on the same day.

Regeneron Pharmaceuticals and Bayer have developed and are marketing Eylea (aflibercept). Eylea patents are due to run out from 2023 to 2032.

Aflibercept is a recombinant fusion protein consisting of portions of human VEGF receptors 1 and 2 extracellular domains fused to the Fc portion of human IgG1 formulated as an iso-osmotic solution for intravitreal administration. Aflibercept is a dimeric glycoprotein with a protein molecular weight of 97 kilodaltons (kDa) and contains glycosylation, constituting an additional 15% of the total molecular mass, resulting in a total molecular weight of 115 kDa. Aflibercept is produced in recombinant Chinese hamster ovary (CHO) cells.

Vascular endothelial growth factor-A (VEGF-A) and placental growth factor (PLGF) are members of the VEGF family of angiogenic factors that can act as mitogenic, chemotactic, and vascular permeability factors for endothelial cells. VEGF acts via two receptor tyrosine kinases, VEGFR-1 and VEGFR-2, present on the surface of endothelial cells. PLGF binds only to VEGFR-1, which is also present on the surface of leucocytes. Activation of these receptors by VEGF-A can result in neovascularization and vascular permeability. Aflibercept acts as a soluble decoy receptor that binds VEGF-A and PLGF, and thereby can inhibit the binding and activation of these cognate VEGF receptors.

The EYLEA safety and efficacy profile is supported by a robust body of research that includes eight pivotal Phase 3 trials, 10 years of real-world experience and more than 50 million EYLEA injections globally. EYLEA (aflibercept) Injection 2 mg (0.05 mL) is indicated for the treatment of patients with Neovascular (Wet) Age-related Macular Degeneration (AMD), Macular Edema following Retinal Vein Occlusion (RVO), Diabetic Macular Edema (DME), and Diabetic Retinopathy (DR).

Biosimilars are follow-on versions of biopharmaceuticals, for which exclusivity has expired. They are approved via stringent regulatory pathways in highly regulated markets (such as EU, US, Japan, Canada, Australia) based on proven similarity of the biosimilar with the originator biopharmaceutical reference product.