Overview
11 DESCRIPTION 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 and contains glycosylation, constituting an additional 15% of the total molecular mass, resulting in a total...
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action 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. 12.
Indications
- 1 INDICATIONS AND USAGE EYLEA HD is indicated for the treatment of: EYLEA HD is a vascular endothelial growth factor (VEGF) inhibitor indicated for the treatment of patients with: Neovascular (Wet) Age-Related Macular Degeneration (nAMD) ( 1.1 ) Diabetic Macular Edema (DME) ( 1.2 ) Diabetic Retinopathy (DR) ( 1.3 ) Macular Edema Following Retinal Vein Occlusion (RVO) ( 1.4 ) 1.1 Neovascular (Wet) Age-Related Macular Degeneration (nAMD) 1.2 Diabetic Macular Edema (DME) 1.3 Diabetic Retinopathy (DR) 1.4 Macular Edema Following Retinal Vein Occlusion (RVO)
Common Doses
- 8 mg
- 0.07 mL
- 114.3 mg
Dosage
2 DOSAGE AND ADMINISTRATION Neovascular (Wet) Age-Related Macular Degeneration (nAMD) The recommended dose for EYLEA HD is 8 mg (0.07 mL of 114.3 mg/mL solution) administered by intravitreal injection every 4 weeks (approximately every 28 days +/- 7 days) for the first three doses, followed by 8 mg (0.07 mL of 114.3 mg/mL solution) via intravitreal injection once every 8 to 16 weeks, +/- 1 week. ( 2.2 ) Some patients did not maintain a response with 8 mg once every 8 to 16 weeks, +/- 1 week, after successful response to the three initial monthly doses.
Contraindications
- 4 CONTRAINDICATIONS Ocular or periocular infection ( 4.1 ) Active intraocular inflammation ( 4.2 ) Hypersensitivity ( 4.3 ) 4.1 Ocular or Periocular Infections EYLEA HD is contraindicated in patients with ocular or periocular infections. 4.2 Active Intraocular Inflammation EYLEA HD is contraindicated in patients with active intraocular inflammation. 4.3 Hypersensitivity EYLEA HD is contraindicated in patients with known hypersensitivity to aflibercept or any of the excipients in EYLEA HD.
Side Effects
- 6 ADVERSE REACTIONS The following potentially serious adverse reactions are described elsewhere in the labeling: Hypersensitivity [see Contraindications (4.3) ] Endophthalmitis, Retinal Detachments, and Retinal Vasculitis with or without Occlusion [see Warnings and Precautions (5.1) ] Increase in intraocular pressure [see Warnings and Precautions (5.2) ] Thromboembolic events [see Warnings and Precautions (5.3) ] The most common adverse reactions (≥3%) reported in patients treated with EYLEA HD were cataract, conjunctival hemorrhage, corneal epithelium defect, intraocular pressure increased,...
Interactions
- No major interactions listed on the FDA label. Always consult a healthcare professional.