Skip to Content

Aflibercept (Ophthalmic)

Medically reviewed by Drugs.com. Last updated on Nov 19, 2020.

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, Intravitreal [preservative free]:

Eylea: 2 mg/0.05 mL (0.05 mL)

Solution Prefilled Syringe, Intravitreal [preservative free]:

Eylea: 2 mg/0.05 mL (0.05 mL)

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

Age-related macular degeneration: Treatment of neovascular (wet) age-related macular degeneration.

Diabetic macular edema: Treatment of diabetic macular edema.

Diabetic retinopathy: Treatment of diabetic retinopathy.

Macular edema: Treatment of macular edema following retinal vein occlusion.

Contraindications

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

Dosing: Adult

Age-related macular degeneration: 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). 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). Some patients may also be treated every 12 weeks (3 months) after one year of effective treatment (not as effective as every 8 week administration).

Diabetic macular edema: 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 of therapy (first 5 injections).

Diabetic retinopathy: 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 of therapy (first 5 injections).

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

Dosing: Geriatric

Refer to adult dosing.

Reconstitution

Prefilled syringe: Each prefilled syringe should only be used for the treatment of a single eye. Syringe tray should be opened under sterile conditions. Twist off syringe cap, then attach a 30-gauge 1/2-inch needle (not supplied) onto the prefilled syringe. Expel air bubbles and slowly depress plunger to expel excess medication (plunger tip should align with the black dosing line on syringe). Refer to manufacturer's labeling for additional information.

Vial: Each vial should only be used for the treatment of a single eye. Remove contents from vial using the supplied 5 micron (19-gauge 11/2-inch) filter needle and 1 mL syringe. Discard filter needle and replace with the supplied 30-gauge 1/2-inch needle (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). Refer to manufacturer's labeling for additional information.

Administration

For ophthalmic intravitreal injection under controlled aseptic conditions. Each vial or prefilled syringe should only be used for the treatment of a single eye. If the contralateral eye requires treatment, a new vial or prefilled syringe 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. Should be administered using a 30-gauge 1/2-inch sterile needle. 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.

Drug Interactions

There are no known significant interactions.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

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

1% to 10%:

Cardiovascular: Arterial thrombosis (2% to 6%)

Central nervous system: Foreign body sensation of eye (3% to 4%)

Immunologic: Antibody development (1% to 3%)

Local: Pain at injection site (1% to 3%), bleeding at injection site (≤2%)

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

<1%, postmarketing, and/or case reports: Endophthalmitis, hypersensitivity reaction

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 rash, pruritus, urticaria, severe anaphylactic/anaphylactoid reactions, or 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 dosing of 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.

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; signs/symptoms of hypersensitivity reaction.

Evaluate pregnancy status prior to use in females of reproductive potential.

Reproductive Considerations

Evaluate pregnancy status prior to use in females of reproductive potential. Women of reproductive potential should use effective contraception prior to initial dose, during treatment, and for at least 3 months after the last intravitreal injection.

Pregnancy Considerations

Aflibercept (ophthalmic) is a vascular endothelial growth factor (VEGF) inhibitor; VEGF is required to achieve and maintain normal pregnancies. Reports of intravitreal VEGF inhibitor use in pregnancy are limited and information specific to use of aflibercept (ophthalmic) has not been located (Peracha 2016). Based on studies in nonpregnant adults, VEGF inhibitors can alter systemic concentrations of VEGF and placental growth factor following intravitreal administration (Peracha 2016; Zehtner 2015). Until additional information is available, intravitreal use during the first trimester should be avoided and use later in pregnancy should be based on patient specific risks versus benefits (Peracha 2016; Polizzi 2015).

Patient Education

What is this drug used for?

• It is used to treat macular degeneration.

• It is used to treat macular swelling.

• It is used to treat some eye problems caused by diabetes.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Floater in the eye

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight

• Swelling, warmth, numbness, change of color, or pain in a leg or arm

• Chest pain

• Jaw pain

• Vision changes

• Eye pain

• Severe eye irritation

• Eye redness

• Eyelid swelling

• Sensitivity to light

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.