[Aflibercept. An approach to pharmacology]

Area of Science:

• Ophthalmology
• Pharmacology
• Biochemistry

Background:

• Vascular Endothelial Growth Factor (VEGF) and placental growth factor (PIGF) play critical roles in ocular neovascularization and inflammation.
• Existing anti-VEGF therapies have varying efficacy and safety profiles.

Purpose of the Study:

• To describe the structure, mechanism of action, and clinical profile of aflibercept.
• To compare aflibercept's affinity and potential efficacy with other anti-VEGF agents.

Main Methods:

• Aflibercept is a recombinant fusion protein combining IgG constant fragment with VEGF receptor domains.
• Intravitreal administration and pharmacokinetic analysis were considered.

Main Results:

• Aflibercept binds to VEGF-A, VEGF-B, and PlGF with high affinity, exceeding that of ranibizumab and bevacizumab.
• Intravitreal aflibercept demonstrates an intraocular anti-inflammatory effect.
• Systemic adverse effects, such as hypertension, are minimal due to low plasma concentrations.

Conclusions:

• Aflibercept's high affinity and dual-targeting (VEGF/PlGF) contribute to its efficacy.
• The drug's favorable safety profile and prolonged intraocular half-life allow for convenient dosing regimens.
• Aflibercept represents a significant advancement in the treatment of ocular diseases driven by VEGF and PlGF.