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Aflibercept (Ophthalmic)

Pronunciation

(a FLIB er sept)

Index Terms

  • AVE 0005
  • AVE 005
  • AVE-0005
  • VEGF Trap
  • VEGF Trap-Eye

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Intraocular [preservative free]:

Eylea: 2 mg/0.05 mL (0.05 mL) [contains mouse (murine) and/or hamster protein]

Brand Names: U.S.

  • Eylea

Pharmacologic Category

  • Ophthalmic Agent
  • Vascular Endothelial Growth Factor (VEGF) Inhibitor

Pharmacology

Aflibercept is a recombinant fusion protein that acts as a decoy receptor for vascular endothelial growth factor-A (VEGF-A) and placental growth factor (PLGF). Aflibercept binds to VEGF-A and PLGF and inhibits binding and activating of endothelial cell receptors, thereby suppressing neovascularization and slowing vision loss.

Absorption

Low levels are detected in the serum following intravitreal injection; levels undetectable 2 weeks after administration .

Distribution

~6 L (IV)

Half-Life Elimination

Plasma: ~5 to 6 days (IV)

Use: Labeled Indications

Diabetic retinopathy: Treatment of diabetic retinopathy in patients with diabetic macular edema

Macular degeneration: Treatment of neovascular (wet) age-related macular degeneration (AMD)

Macular edema: Treatment of macular edema following retinal vein occlusion (RVO) and diabetic macular edema

Contraindications

Hypersensitivity to aflibercept or any component of the formulation; current ocular or periocular infection; active intraocular inflammation

Dosing: Adult

Age-related macular degeneration (AMD): Intravitreal: 2 mg (0.05 mL) once every 4 weeks (monthly) for the first 12 weeks (3 months), followed by 2 mg (0.05 mL) once every 8 weeks (every 2 months) thereafter. Although may be administered every 4 weeks, additional efficacy has not been demonstrated (compared with every 8 week administration); some patients may require every 4 week (monthly) dosing after the first 12 weeks of therapy (first 3 injections).

Canadian labeling: After the first 12 months, the treatment interval may be extended up to every 12 weeks (3 months) based on visual and/or anatomic outcomes and with regular evaluation.

Diabetic macular edema (DME): Intravitreal: 2 mg (0.05 mL) once every 4 weeks (monthly) for the first 5 injections, followed by 2 mg (0.05 mL) once every 8 weeks (every 2 months). Although may be administered every 4 weeks, additional efficacy has not been demonstrated (compared with every 8 week administration); some patients may require every 4 week (monthly) dosing after the first 20 weeks (first 5 injections).

Diabetic retinopathy (DR) in patients with DME: Intravitreal: 2 mg (0.05 mL) once every 4 weeks (monthly) for the first 5 injections, followed by 2 mg (0.05 mL) once every 8 weeks (every 2 months). Although may be administered every 4 weeks, additional efficacy has not been demonstrated (compared with every 8 week administration); some patients may require every 4 week (monthly) dosing after the first 20 weeks (first 5 injections).

Macular edema following retinal vein occlusion (RVO): Intravitreal: 2 mg (0.05 mL) once every 4 weeks (monthly)

Canadian labeling: The dosing interval should not be <4 weeks but may be extended up to every 12 weeks (3 months) based on visual and anatomic outcomes; assess the need for continued therapy every 1 to 2 months. In studies, after 24 weeks (6 months), the interval was extended based on visual and anatomic outcomes for central retinal vein occlusion and extended to once every 8 weeks for branch retinal vein occlusion.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

No dosage adjustment necessary.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); however, no adjustment expected due to minimal systemic absorption.

Reconstitution

Each vial should only be used for the treatment of a single eye. If the contralateral eye requires treatment, a new vial should be used and the sterile field, syringe, gloves, drapes, eyelid speculum, filter, and injection needles should be changed before aflibercept is administered to the other eye. Inspect vial prior to administration; do not use if particulates, cloudiness, or discoloration are present.

Administration

For ophthalmic intravitreal injection only. Using aseptic technique, remove entire contents of vial using a 5 micron, 19-gauge 11/2 inch filter needle (supplied) attached to a 1 mL syringe (supplied); keep the needle bevel submerged to avoid introducing excess air. Draw plunger rod back to completely empty the filter needle, then remove and discard filter needle and replace with a sterile 30-gauge 1/2 inch needle (supplied) for intravitreal injection procedure (do not use filter needle for intravitreal injection). Expel air bubbles and slowly depress plunger to expel excess medication (plunger tip should align with the 0.05 mL marking on syringe). The intravitreal injection should be performed under controlled aseptic conditions, which include surgical hand disinfection and the use of sterile gloves, a sterile drape, and a sterile eyelid speculum (or equivalent). Adequate anesthesia and a topical broad-spectrum antimicrobial agent should be administered prior to the procedure.

Storage

Store refrigerated at 2°C to 8°C (36°F to 46°F). Do not freeze. Protect from light. Store in original container prior to use. Discard unused product. The Canadian labeling indicates that prior to usage, the unopened vial may be stored at room temperature (25°C) for up to 24 hours.

Drug Interactions

There are no known significant interactions.

Adverse Reactions

>10%: Ophthalmic: Conjunctival hemorrhage (12% to 31%), cataract (5% to 19%), eye pain (9% to 13%)

1% to 10%:

Cardiovascular: Arterial thrombosis (2% to 6%)

Central nervous system: Foreign body sensation of eye (3%)

Immunologic: Antibody development (1% to 3%)

Local: Pain at injection site (1% to 3%), bleeding at injection site (≤1%)

Ophthalmic: Increased intraocular pressure (2% to 9%), vitreous detachment (2% to 8%), vitreous opacity (1% to 8%), epithelial keratopathy (4% to 7%), ocular hyperemia (4% to 5%), increased lacrimation (3% to 4%), retinal pigment epithelium detachment (3%), intraocular inflammation (2% to 3%), retinal pigment epithelium tear (2%), blurred vision (1% to 2%), eyelid edema (1% to 2%), corneal edema (≤1%)

<1% (Limited to important or life-threatening): Anterior chamber inflammation, endophthalmitis, hyalitis, hypersensitivity, hypopyon, iatrogenic traumatic cataract, iridocyclitis, iritis, retinal detachment, retinal hole without detachment, uveitis

Warnings/Precautions

Concerns related to adverse effects:

• Endophthalmitis/retinal detachment: Intravitreous injections are associated with endophthalmitis, retinal detachments, retinal tear, retinal pigment epithelium tear, and cataract, including traumatic cataract. Use proper aseptic injection techniques. Instruct patients to report any signs of infection (eg, eye pain or redness, photophobia, blurred vision) immediately; manage appropriately.

• Hypersensitivity reactions: Hypersensitivity may present as severe intraocular inflammation.

• Increased intraocular pressure: Following intravitreal injection, intraocular pressure may increase (acute). Onset is seen within 60 minutes. Sustained increases in intraocular pressure have also been reported (with repeated intravitreal VEGF inhibitors). Monitor intraocular pressure and optic nerve head perfusion.

• Thromboembolic events: Risk of thromboembolic events (eg, nonfatal stroke/MI, vascular death) may be increased following intravitreal administration of VEGF inhibitors, including aflibercept.

Special populations:

• Women: Women of reproductive potential should use effective contraception prior to initial dose, during treatment, and for ≥3 months after the last dose.

Monitoring Parameters

Intraocular pressure immediately following injection; signs of infection/inflammation (for first week following injection); optic nerve head perfusion; signs/symptoms of endophthalmitis or retinal detachment; visual acuity

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies. Women of reproductive potential should use effective contraception prior to initial dose, during treatment, and for ≥3 months after the last dose.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience floater in the eye. Have patient report immediately to prescriber signs of severe cerebrovascular disease (change in strength on one side is greater than the other, difficulty speaking or thinking, change in balance, or vision changes), signs of DVT (edema, warmth, numbness, change in color, or pain in the extremities), angina, jaw pain, vision changes, eye pain, severe eye irritation, eye redness, eyelid edema, or sensitivity to light (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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