Aflibercept

Name: Aflibercept

Description

EYLEA (aflibercept) 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 formulated as an iso-osmotic solution for intravitreal administration. Aflibercept is a dimeric glycoprotein with a protein molecular weight of 97 kilodaltons (kDa) and contains glycosylation, constituting an additional 15% of the total molecular mass, resulting in a total molecular weight of 115 kDa. Aflibercept is produced in recombinant Chinese hamster ovary (CHO) cells.

EYLEA is a sterile, clear, and colorless to pale yellow solution. EYLEA is supplied as a preservative-free, sterile, aqueous solution in a single-use, glass vial designed to deliver 0.05 mL  (50 microliters) of EYLEA (40 mg/mL in 10 mM sodium phosphate, 40 mM sodium chloride, 0.03% polysorbate 20, and 5% sucrose, pH 6.2).

Inform MD

Before receiving aflibercept, tell your doctor about all your medical conditions including if you:

  • have an infection in or around your eye(s)
  • have had a blood clot or stroke
  • are allergic to any medication, food, or dyes
  • are pregnant or breastfeeding

Tell your doctor about all the medications you take including prescription and non-prescription medications, vitamins, and herbal supplements.

Aflibercept Overdose

If aflibercept is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

Cautions for Aflibercept

Contraindications

  • Ocular or periocular infections.1

  • Active intraocular inflammation.1

  • Known hypersensitivity (e.g., severe intraocular inflammation) to aflibercept or any ingredient in the formulation.1

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity reactions reported.1 (See Contraindications under Cautions.)

Endophthalmitis and Retinal Detachment

Intravitreal injections, including with aflibercept, associated with endophthalmitis and retinal detachment.1 Always use proper aseptic injection technique.1

If signs or symptoms of endophthalmitis or retinal detachment (e.g., redness, sensitivity to light, pain, changes in vision [including blurred vision]) occur, manage appropriately.1

Increased IOP

Acute increases in IOP observed within 60 minutes of intravitreal injection.1 Sustained increases in IOP also observed following repeated intravitreal injections of VEGF antagonists.1 Monitor IOP and perfusion of optic nerve head and manage appropriately.1

Thromboembolic Events

Potential risk of arterial thromboembolic events following intravitreal injection of VEGF antagonists, including aflibercept.1

Immunogenicity

Incidence of immunoreactivity to aflibercept was similar before and after 24–100 weeks of therapy.1 No differences in efficacy or safety between patients with or without immunoreactivity.1

Specific Populations

Pregnancy

Category C.1

No adequate and well-controlled studies in pregnant women.1 Animal studies suggest a possibility of adverse embryofetal effects.1

Use only if potential benefits justify potential risk to fetus.1 Women of childbearing potential should use effective contraception prior to initiating therapy, during treatment, and for ≥3 months after last intravitreal injection is administered.1

Lactation

Not known whether aflibercept is distributed into milk.1 Use not recommended in nursing women.1 Discontinue nursing or the drug.1

Pediatric Use

Safety and efficacy not established.1

Geriatric Use

No substantial differences in safety or efficacy relative to younger adults.1

Renal Impairment

No differences in plasma concentrations observed with various degrees of renal impairment.1 (See Special Populations under Pharmacokinetics.)

Common Adverse Effects

Conjunctival hemorrhage,1 2 3 eye pain,1 2 3 cataract,1 vitreous detachment,1 2 3 vitreous floaters,1 2 increased IOP.1 2 3

What is aflibercept ophthalmic (eylea)?

Aflibercept is made from a human antibody fragment. It works by keeping new blood vessels from forming under the retina (a sensory membrane that lines the inside of the eye). In people with a certain type of eye disease, new blood vessels grow under the retina where they leak blood and fluid. This is known as the "wet form" of macular degeneration.

Aflibercept ophthalmic (for the eyes) is used to treat wet age-related macular degeneration. Aflibercept is also used to treat swelling in the retina caused by a blockage in the blood vessels.

Aflibercept ophthalmic may also be used for purposes not listed in this medication guide.

What is the most important information i should know about aflibercept ophthalmic (eylea)?

Aflibercept ophthalmic (for the eyes) is used to treat wet age-related macular degeneration. Aflibercept is also used to treat swelling in the retina caused by a blockage in the blood vessels.

You should not use aflibercept if you have swelling inside your eyes, or any type of infection (bacterial, fungal, viral) in or around your eyes.

'Call your doctor at once if you have eye pain or redness, swelling or puffiness around your eyes, or sudden vision problems at any time during treatment.

Usual Adult Dose for Macular Edema

Macular edema following retinal vein occlusion (RVO):
2 mg (0.05 mL) administered by intravitreal injection once every 4 weeks (monthly).

Diabetic Macular Edema (DME)/Diabetic Retinopathy (DR) in Patients with DME:
2 mg (0.05 mL) administered by intravitreal injection every 4 weeks (monthly) for the first 5 injections, followed by 2 mg (0.05 mL) via intravitreal injection once every 8 weeks (2 months).

Comments: Additional efficacy was not demonstrated when dosed every 4 weeks compared to every 8 weeks.

Other Comments

Reconstitution/preparation techniques:
-Refer to the manufacturer product information for preparation instructions.
-The product should be inspected visually prior to administration. If particulates, cloudiness, or discoloration are visible, the vial should not be used.
-The intravitreal injection procedure should be carried out 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 microbicide should be given prior to the injection.
-Immediately following the intravitreal injection, patients should be monitored for elevation in intraocular pressure. Appropriate monitoring may consist of a check for perfusion of the optic nerve head or tonometry. If required, a sterile paracentesis needle should be available.
-Following intravitreal injection, patients should be instructed to report any symptoms suggestive of endophthalmitis or retinal detachment (e.g., eye pain, redness of the eye, photophobia, blurring of vision).
-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. -After injection, any unused product should be discarded.

Patient advice:
-In the days following administration, patients are at risk of developing endophthalmitis or retinal detachment. If the eye becomes red, sensitive to light, painful, or develops a change in vision, patients should seek immediate care from an ophthalmologist.
-Patients may experience temporary visual disturbances after an intravitreal injection and the associated eye examinations. Patients should be advised not to drive or use machinery until visual function has recovered sufficiently.
-Intravitreal aflibercept has minor influence on the ability to drive and use machines due to possible temporary visual disturbances. Patients should not drive or use machines until their visual function has recovered sufficiently.

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