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Pharmacologic class: Vascular endothelial growth factor (VEGF) inhibitor

Therapeutic class: Ophthalmic agent

Pregnancy risk category C


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.


Solution for ophthalmic injection: 40 mg/ml in 3-ml (0.278-ml fill) single-use vials

Indications and dosages

Neovascular (wet) age-related macular degeneration

Adults: 2 mg (0.05 ml) by intravitreal injection into affected eye q 4 weeks for the first 3 months, followed by 2 mg (0.05 ml) once q 8 weeks


• Hypersensitivity to drug or its components
• Ocular or periocular infection
• Active intraocular inflammation


Use cautiously in:
• pregnant or breastfeeding patients
• children (safety and efficacy not established).


• Be aware that drug should be administered by ophthalmic intravitreal injection only under controlled aseptic conditions by a qualified health care professional.
• Provide adequate anesthesia and a topical broad-spectrum anti-infective before the injection, as prescribed.
• Inspect drug for particulate matter and discoloration before administering.
• Use a filter needle to draw up the prescribed dose; remove the filter needle from syringe, and attach a 30G, ½-inch injection needle for the intravitreal injection. Discard unused drug after injection.
• Be aware that each vial should only be used for the treatment of a single eye. If the contralateral eye requires treatment, use a new vial and change all equipment.
• Immediately following the intravitreal injection, assess patient for increased intraocular pressure (IOC).

Adverse reactions

CNS: nonfatal stroke

CV: nonfatal MI, vascular death

EENT: conjunctival hyperemia, conjunctival hemorrhage, eye pain, cataract, vitreous detachment, vitreous floaters, increased IOC, endophthalmitis, corneal erosion, corneal edema, retinal detachment, retinal tear, retinal pigment epithelium tear, injection-site pain, injection-site hemorrhage, foreign body sensation in eye, increased lacrimation, blurred vision, eyelid edema

Other: hypersensitivity



Patient monitoring

• Continue to monitor patient for increased IOP, endophthalmitis, retinal detachment, and arterial thromboembolic events and be prepared to treat appropriately.

Patient teaching

Instruct patient to contact ophthalmologist immediately if treated eye becomes red, light sensitive, or painful, or if vision change occurs.

Instruct patient to immediately report signs and symptoms of stroke (such as weakness on one side of body or slurred speech), chest pain, or other new signs and symptoms.
• Caution patient to avoid driving and other hazardous activities until visual function has recovered sufficiently.
• As appropriate, review all other significant and life-threatening adverse reactions mentioned above.

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References in periodicals archive ?
The recently launched products the anticoagulant Xarelto , the eye medicine Eylea , the cancer drugs Stivarga and Xofigo , and Adempas to treat pulmonary hypertension continued to experience encouraging growth, posting combined sales of EUR 1,082 million (Q3 2014: EUR 750 million).
Sales of EYLEA (Regeneron/Bayer), which also targets VEGF-A but not VEGF-C first marketed in November 2011 for the treatment of wet AMD, were over $US1.
The drug, aflibercept (marketed as Eylea or Zaltrap), is used to treat metastatic colorectal cancer and a form of macular degeneration.
In fact, less than 20 percent of patients are currently treated with Lucentis or Regeneron's Eylea (approved for wet AMD and central RVO but not DME) -- highlighting cost and managed care coverage as obstacles within the diabetic ophthalmology market.
Third quarter 2015 EYLEA (aflibercept) Injection global net sales increased 53% to $1.
EYLEA is now also approved for the treatment of visual impairment due to myopic choroidal neovascularization (myopic CNV).
Eylea acts as a VEGF inhibitor and is approved for the treatment of wAMD and ME-CRVO in all 7MM, and for DME in the US and EU.
GlobalData analyst for neurology and ophthalmology, Catherine Daly, said: "The global AMD treatment market is overwhelmingly dominated by anti-vascular endothelial growth factor (anti-VEGF) drugs, including Lucentis, Avastin, and Eylea, which together accounted for 98% of sales for AMD in 2013.
A team of ophthalmologists at the University of Iowa has shown that the drug, Eylea, can ease leaking and vision problems for wet AMD patients.
BioTrends Research Group, one of the world's leading research and advisory firms for specialized biopharmaceutical issues, finds that, nine months after commercial availability in the US, Regeneron's Eylea captures 13 percent of wet age-related macular degeneration (AMD) patient share, although patient shares for Genentech's Avastin and Lucentis have remained relatively stable compared to one year ago.
In the EU, EYLEA is already approved for the treatment of patients with neovascular (wet) age-related macular degeneration, visual impairment due to diabetic macular edema, and visual impairment due to macular edema secondary to retinal vein occlusion (branch RVO or central RVO).
The results, presented today at the 15th EURETINA Congress (17-20 September, 2015) in Nice, France, showed sustained improvements in best corrected visual acuity (BCVA) at three years, for EYLEA 2 milligrams (mg), compared to laser photocoagulation.