Regeneron Pharmaceuticals has announced that Eylea ( Aflibercept ) injection has been approved by the European Commission for the treatment of patients with neovascular ( wet ) age-related macular degeneration ( wet AMD ).

Vascular Endothelial Growth Factor ( VEGF ) is a naturally occurring protein in the body. Its normal role in a healthy organism is to trigger formation of new blood vessels ( angiogenesis ) supporting the growth of the body's tissues and organs. However, in certain diseases, such as wet age-related macular degeneration, it is also associated with the growth of abnormal new blood vessels in the eye, which exhibit abnormal increased permeability that leads to edema. Scarring and loss of fine-resolution central vision often results.

Eylea 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 and formulated as an iso-osmotic solution for intravitreal administration. EYLEA acts as a soluble decoy receptor that binds VEGF-A and placental growth factor ( PlGF ) and thereby can inhibit the binding and activation of their cognate VEGF receptors.

The recommended dose for Eylea is 2 mg administered by intravitreal injection every 4 weeks ( monthly ) for the first 12 weeks ( 3 months ), followed by 2 mg once every 8 weeks ( 2 months ).
Although Eylea may be dosed as frequently as 2 mg every 4 weeks ( monthly ), additional efficacy was not demonstrated when Eylea was dosed every 4 weeks compared to every 8 weeks.

Important safety information

Eylea injection is contraindicated in patients with ocular or periocular infections, active intraocular inflammation, or known hypersensitivity to Aflibercept or to any of the excipients.

Intravitreal injections, including those with Eylea, have been associated with endophthalmitis and retinal detachments. Proper aseptic injection technique must always be used when administering Eylea. Patients should be instructed to report any symptoms suggestive of endophthalmitis or retinal detachment without delay and should be managed appropriately.
Intraocular inflammation has been reported during the post approval use of Eylea.
Acute increases in intraocular pressure have been seen within 60 minutes of intravitreal injection, including with Eylea. Sustained increases in intraocular pressure have also been reported after repeated intravitreal dosing with VEGF inhibitors. Intraocular pressure and the perfusion of the optic nerve head should be monitored and managed appropriately.
There is a potential risk of arterial thromboembolic events ( ATEs ) following use of intravitreal VEGF inhibitors, including Eylea, defined as non-fatal stroke, non-fatal myocardial infarction, or vascular death ( including deaths of unknown cause ). The incidence of ATEs in the VIEW 1 and VIEW 2 wet AMD trials in patients treated with Eylea was 1.8% during the first year.

The most common adverse reactions ( 5% or more ) reported in patients receiving Eylea were conjunctival hemorrhage, eye pain, cataract, vitreous detachment, vitreous floaters, and increased intraocular pressure.

Serious adverse reactions related to the injection procedure have occurred in less than 0.1% of intravitreal injections with Eylea including endophthalmitis, traumatic cataract, increased intraocular pressure and vitreous detachment.

Source: Regeneron, 2012

XagenaMedicine2012