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Medical Areas: Ophthalmology | Family Medicine | Infections and Infectious Diseases | Genetic Disease
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The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
Company: Regeneron Pharmaceuticals
Approval Status: Approved November 2011
Treatment Area: neovascular (wet) age-related macular degeneration
Eylea (aflibercept) is a recombinant fusion protein consisting of portions of human . Vascular endothelial growth (VEGF) receptors 1 and 2. VEGF-A is a member 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. Activation of these receptors by VEGF-A can result in neovascularization and vascular permeability.
Eylea is specifically approved for neovascular (wet) age-related macular degeneration.
Eylea is supplied as a solution for intravitreal injection. The recommended dose is 2 mg (0.05 mL or 50 microliters) administered by intravitreal injection every four weeks (monthly) for the first 12 weeks (three months), followed by 2 mg
(0.05 mL) via intravitreal injection once every 8 weeks (two months).
The FDA Approval of Eylea was based on two randomized, multi-center, double-masked, active-controlled studies, VIEW1 and VIEW2. A total of 2,412 subjects were treated and evaluable for efficacy. The subjects were randomized to one of four dosing regimens: 1) Eylea administered 2 mg every 8 weeks following three initial monthly doses (Eylea 2Q8); 2) Eylea administered 2 mg every four weeks (Eylea 2Q4); 3) Eylea 0.5 mg administered every four weeks (Eylea 0.5Q4); and 4) ranibizumab administered 0.5 mg every four weeks (ranibizumab 0.5 mg Q4). The primary efficacy endpoint was the proportion of subjects who maintained vision, defined as losing fewer than 15 letters of visual acuity at week 52 compared to baseline. Both Eylea 2Q8 and 2Q4 groups were shown to have efficacy that was clinically equivalent to the ranibizumab 0.5 mg Q4 group. In VIEW1 this endpoint was reached by 94%, 95% and 94% of subjects in the Eylea 2Q8, Eylea 2Q4 and ranibizumab arms, respectively. In VIEW2 this endpoint was reached by 95% of subjects in all three treatment arms.
Adverse events associated with the use of Eylea may include, but are not limited to, the following:
- conjunctival hemorrhage
- eye pain
- vitreous detachment
- vitreous floaters
- increased intraocular pressure
Mechanism of Action
Eylea (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. Vascular endothelial growth factor-A (VEGF-A) is a member 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. Activation of these receptors by VEGF-A can result in neovascularization and vascular permeability.
Heier JS, Boyer D, Nguyen QD, Marcus D, Roth DB, Yancopoulos G, Stahl N, Ingerman A, Vitti R, Berliner AJ, Yang K, Brown DM; CLEAR-IT 2 Investigators The 1-year results of CLEAR-IT 2, a phase 2 study of vascular endothelial growth factor trap-eye dosed as-needed after 12-week fixed dosing. Ophthalmology 2011 Jun;118(6):1098-106
Brown DM, Heier JS, Ciulla T, Benz M, Abraham P, Yancopoulos G, Stahl N, Ingerman A, Vitti R, Berliner AJ, Yang K, Nguyen QD; CLEAR-IT 2 Investigators Primary endpoint results of a phase II study of vascular endothelial growth factor trap-eye in wet age-related macular degeneration. Ophthalmology 2011 Jun;118(6):1089-97
Nguyen QD, Shah SM, Browning DJ, Hudson H, Sonkin P, Hariprasad SM, Kaiser P, Slakter JS, Haller J, Do DV, Mieler WF, Chu K, Yang K, Ingerman A, Vitti RL, Berliner AJ, Cedarbaum JM, Campochiaro PA A phase I study of intravitreal vascular endothelial growth factor trap-eye in patients with neovascular age-related macular degeneration. Ophthalmology 2009 Nov;116(11):2141-8.e1
For additional information regarding Eylea or neovascular (wet) age-related macular degeneration, please visit the Eylea web page.