Aflibercept · intravitreal injection
Injections & Implants
Approved uses
Neovascular (wet) age-related macular degeneration
2 mg (0.05 mL of 40 mg/mL) intravitreally every 4 weeks for 3 months, then every 8 weeks
Every-4-week dosing gave no added efficacy over every-8-week in most patients after loading
Diabetic macular edema and diabetic retinopathy
2 mg (0.05 mL of 40 mg/mL) intravitreally every 4 weeks for the first 5 injections, then every 8 weeks
One regimen covers both; the label treats them together
Macular edema following retinal vein occlusion
2 mg (0.05 mL of 40 mg/mL) intravitreally every 4 weeks
Retinopathy of prematurity
0.4 mg (0.01 mL of 40 mg/mL) intravitreally; may be given bilaterally the same day and repeated in each eye
The only indication at a different strength, one fifth the adult dose
Contraindications
Ocular or periocular infection Active intraocular inflammation Hypersensitivity.
Intravitreal injection, pre-filled syringe and single-dose vial, 40 mg/mL; 2 mg (0.05 mL) for adult indications and 0.4 mg (0.01 mL) for retinopathy of prematurity. Single eye use only.
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.
Warnings & Precautions
Endophthalmitis, retinal detachment, and retinal vasculitis with or without occlusion may follow intravitreal injection; instruct patients to report any suggestive symptoms without delay. Acute intraocular inflammation and increases in intraocular pressure have been reported. There is a theoretical risk of arterial thromboembolic events after intravitreal VEGF inhibition.
Common Side Effects
The most common adverse reactions (≥5%) reported in patients receiving EYLEA were conjunctival hemorrhage, eye pain, cataract, vitreous detachment, vitreous floaters, and intraocular pressure increased.
Pregnancy: No adequate and well-controlled studies in pregnant women. Aflibercept caused external, visceral, and skeletal malformations in rabbits at systemic exposures above those expected after intravitreal dosing. Advise a woman of reproductive potential to use effective contraception during treatment and for a period after the last dose.
Lactation: No data on presence in human milk or effects on the breastfed infant; consider the mother's clinical need alongside any potential adverse effect.
The safety and effectiveness of EYLEA have been demonstrated in two clinical studies of pre-term infants with ROP. These two studies randomized pre-term infants between initial treatment with EYLEA or laser.