EYLEA (aflibercept) belongs to a class of drugs called vascular endothelial growth factor (VEGF) antagonists and is used to treat “wet” age-related macular degeneration (AMD) and other eye conditions. Wet AMD is characterized by the growth of abnormal blood vessels in the eye, which can leak and subsequently lead to vision loss. EYLEA works by helping prevent the growth of these abnormal blood vessels. In this article, we answer some of the most common questions about EYLEA.
- What is EYLEA?
- How does EYLEA work?
- What is EYLEA used for?
- What is the difference between aflibercept and ziv-aflibercept?
- How is EYLEA administered?
- Do eye injections hurt?
- Does EYLEA interact with other medications?
- Who should not take EYLEA?
- For how long do I need to receive EYLEA injections for macular degeneration?
- What are the side effects of EYLEA?
- Can I drive while taking EYLEA?
- What are possible alternatives to EYLEA?
1. What is EYLEA?
EYLEA is the brand name for aflibercept, a drug that comes in the form of a liquid that is injected into the eye to treat wet age-related macular degeneration (wet AMD), macular edema (the build-up of fluids that causes swelling in the edema) following retinal vein occlusion (MEfRVO), diabetic retinopathy (DR), and diabetic macular edema (DME).
EYLEA belongs to a class of drugs called vascular endothelial growth factor (VEGF) antagonists. VEGF is a protein that is a major contributor to the growth or protrusion of blood vessels (processes called neovascularization and angiogenesis), so blocking it from working helps prevent the growth of abnormal blood vessels that characterizes wet AMD. This is why EYLEA is also called as an anti-angiogenesis drug. This mechanism of action has been found to slow the progression of macular edema.
EYLEA is usually administered once per month initially. In most cases (depending on the condition being treated and your response to the treatment), your doctor will change your regimen to one injection every 8 weeks, usually after the first 3 months of treatment. Injections are given by your doctor.
EYLEA treatment aims to maintain (and even restore) vision. Because of how EYLEA works, it is also referred to as anti-VEGF treatment or therapy.
2. How does EYLEA work?
EYLEA works by blocking vascular endothelial growth factor (VEGF), a protein that contributes to the growth of blood vessels. Normally, VEGF is a healthy and important molecule, but in conditions relating that are characterized by leaking and swelling of blood vessels in the macular (a part of the eye below the central part of the retina that is responsible for sharp, central eyesight necessary for activities such as reading), its activity makes symptoms worse.
EYLEA prevents VEGF (A and B) from working by blocking it from “binding” its receptors (called VEGFR1 and VEGFR2), as well as blocking placental growth factor (PIGF). Treatment with EYLEA is often referred to as anti-VEGF therapy.
EYLEA does this by acting as a decoy receptor with a greater binding affinity (the proteins are more likely to bind to it) than the body’s natural receptors.
This mechanism of action is different from other anti-VEGF drugs, including Lucentis (ranibizumab), which is a monoclonal antibody fragment (designed to replicate your immune system’s antibodies). Because of the different mechanism of action, patients who fail to respond to one therapy may respond to another.
3. What is EYLEA used for?
EYLEA has been approved by the FDA to treat the following conditions:
EYLEA for Wet AMD
Age-related macular degeneration (AMD) is a common eye condition that usually begins affecting people in their 50s or 60s. It can lead to vision loss and blurriness in the middle part of your vision. “Dry” AMD is more common and can lead to vision loss over several years. “Wet” AMD is the more serious form of the condition and can lead to vision loss in a matter of weeks or months.
It is called wet AMD because of blood vessels in the eye leaking fluids (such as blood, lipids, and serum) into the macular. Vascular endothelial growth factor (VEGF) contributes to the growth of abnormal and weak blood vessels that are often responsible for leaking fluids.
Because of how EYLEA works (as described in the previous question: How does EYLEA work?), it helps prevent the growth of blood vessels and the subsequent leaking from occurring.
According to the NHS, EYLEA prevents vision from getting worse in 9 out of every 10 patients and improves vision in 3 out of every 10 patients.
Treatment for wet AMD usually consists of one 0.05 mL injection of EYLEA solution (containing 2 mg of the active ingredient, aflibercept) per month for the first three months of treatment, followed by one injection every 8 weeks.
EYLEA for Macular Edema following Retinal Vein Occlusion (RVO)
Retinal vein occlusion (RVO) is when blood vessels in the retina are blocked, usually because of a blood clot. Either the main retinal vein is blocked (central retinal vein occlusion (CRVO)) or, more commonly, one or more of the smaller branches (branch retinal vein occlusion (BRVO)).
RVO means blood cannot drain from the retina, which can lead to fluids leaking into the macula and causing inflammation and swelling (edema), hence the name macular edema following retinal vein occlusion (MEfRVO). This can lead to loss or blurring of vision, often suddenly (within hours or days).
Additionally, VEGF has been associated with the growth of abnormal blood vessels in MEfRVO. EYLEA helps treat this in the same way it does wet AMD. Two studies have found that EYLEA can improve eyesight in patients with MEfRVO.
Treatment for MEfRVO usually consists of one 0.05 mL injection of EYLEA solution (containing 2 mg of the active ingredient, aflibercept) per month.
EYLEA for Diabetic Retinopathy (DR) With or Without Diabetic Macular Edema (DME)
Diabetic retinopathy (DR) is a (type 1 or type 2) diabetes complication in which high blood sugar levels cause damage to blood vessels in the retina. When diabetic retinopathy worsens, it can also affect the edema and lead to swelling, which is called diabetic macular edema (DME).
As with MEfRVO, VEGF has been associated with the growth of abnormal blood vessels in cases of DR and DMR. Several studies have found that EYLEA can improve vision in patients with DR either with or without DME.
Treatment for DR and DME usually consists of one 0.05 mL injection of EYLEA solution (containing 2 mg of the active ingredient, aflibercept) per month for the first 5 injections, followed by one injection every 8 weeks.
Please be aware that the conditions EYLEA has been approved to treat, and specific treatment guidelines, may vary in different countries.
4. What is the difference between aflibercept and ziv-aflibercept?
The development of aflibercept resulted in two forms of the drug: aflibercept and ziv-aflibercept. While the two forms are chemically very similar and have the same mechanism of action, there are some key differences. The most notable difference relates to osmolarity, which is the measure of solute concentration per unit volume of solvent (for example, the amount of salt in seawater).
- Administered via intravitreal injection (into the eye)
- Approved for the treatment of eye conditions (see question 3: What is EYLEA used for?)
- Osmolarity of ~250-260 mOsm/kg
- Administered via intravenous injection (into the veins)
- Approved for the treatment of colorectal cancer
- Osmolarity of ~815-820 mOsm/kg
The higher osmolarity of ziv-aflibercept is the most notable chemical difference between the two drugs. It has been suggested that the higher concentration of ziv-aflibercept could lead to retinal toxicity and retinal detachment. It is, therefore, not approved for intravitreal injection to treat eye conditions.
Nonetheless, several studies have investigated the use of ziv-aflibercept in treating eye condition with intravitreal injections. Because it usually costs significantly less than aflibercept and other anti-VEGF drugs, it would be an attractive option in many cases.
For the time being, however, the safety and efficacy of ziv-aflibercept in the treatment of wet AMD and other eye conditions are not established.
5. How is EYLEA administered?
After disinfection and local anesthesia are used on the eye, the injection is administered by a qualified healthcare professional.
EYLEA only comes in one strength, which is a 0.05 mL solution containing 2 mg of the active ingredient (aflibercept).
6. Do eye injections hurt?
Although the thought of eye injections is scary for many people, anesthetic eye drops help ensure they are usually painless.
If you do experience pain, you should speak to your doctor about your options (including different anesthetics).
7. Does EYLEA interact with other medications?
Only a small amount of EYLEA is injected into your eye, meaning very little enters your bloodstream. While this suggests the possibility of drug interactions is low, no drug interaction studies have been performed.
It is highly recommended that you tell your doctor about any medications you take, have taken recently, or plan to take. In particular, it is important to tell your doctor about any other eye treatment you are receiving or have received, such as photodynamic therapy.
8. Who should not take EYLEA?
EYLEA is not be used if:
- If you are allergic to aflibercept or any other ingredients of EYLEA
- You have an infection in or around your eye(s)
You should tell your doctor if:
- You have had a stroke or have had temporary signs of a stroke (weakness or paralysis of the limbs or face, difficulty speaking, or understanding)
- You have glaucoma
- If you are pregnant, think you may be pregnant, or are planning to have a baby. It is not known if EYLEA can harm a developing baby, so an alternative treatment may be preferable
- If you are breastfeeding. It is not known whether EYLEA is excreted in human milk, so an alternative treatment may be recommended for a nursing mother
9. For how long do I need to receive EYLEA injections for macular degeneration?
There is no standard length of time EYLEA therapy lasts in the treatment of wet AMD. Your doctor will likely perform regular evaluations to assess how the treatment is performing. In some cases, your doctor may decide to stop treatment or extend the length of time between injections.
This is usually the case for macular edema following retinal vein occlusion, diabetic retinopathy, and diabetic macular edema as well.
10. What are the side effects of EYLEA?
Eye injections, including those with EYLEA, carry inherent risks. Warnings include:
- Endophthalmitis (inflammation usually caused by infection) and retinal detachments
- Increases in intraocular pressure (the pressure of fluids within the eye) within 60 minutes of the injection being administered
- Thromboembolic events (nonfatal stroke, nonfatal heart attacks, or vascular death)
The risk of serious or fatal adverse events is considered low, particularly for patients who do not have diabetic macular edema or diabetic retinopathy. Nonetheless, your doctor should check your eye pressure and eye health before and after the injection. Additionally, you should contact your doctor immediately if your eye becomes red, sensitive to light, or painful, or if you have a change in vision.
- Bloody eye
- Blurred vision or loss of vision
- Red, sore eyes
- Redness of the white part of the eyes or inside of the eyelids
- Redness, swelling, or itching of the eyelid
- Seeing flashes or sparks of light
- Seeing floating spots before the eyes, or a veil or curtain appearing across a part of your vision
- Vision changes
You should contact your doctor or nurse immediately if you experience any of these less common side effects:
- Bleeding or pain at the injection site
- Swelling of the eyelid
You should contact your doctor or nurse immediately if you experience any of these rare side effects:
- Fast heartbeat
- Hives, itching, rash, or skin redness
- Joint pain, stiffness, or swelling
- Swelling of the eye, face, lips, hands, or feet
- Tightness in the chest
- Trouble breathing or swallowing
You should contact your doctor or nurse immediately if you experience any of these side effects (the incidence of which are unknown):
- Pain in the chest, groin, or legs, especially the calves
- Severe, sudden headache
- Slurred speech
- Sudden loss of coordination
- Sudden, severe weakness or numbness in the arm or leg
Some side effects that do not usually need medical treatment and often go away as your body adjusts to the treatment include:
- Feeling like something is in your eye
- Watery eyes
Signs of a serious allergic reaction should be treated as a medical emergency. They include:
- Skin rash – for example itchy, red, or swollen skin
- Tightness in the chest or throat
- Trouble breathing or talking
- Swollen mouth, face, lips, tongue, or throat
This is not a complete list of the possible side effects of EYLEA. For more information, you should speak to your doctor or read the EYLEA patient information label.
11. Can I drive while taking EYLEA?
It is normally recommended that you do not drive on the day of your injection, as side effects can impair your ability. If you experience any vision problems, do not drive until your vision is back to normal.
In most cases, you are still able to drive while taking EYLEA if your eyesight meets the minimum requirements where you live. In some places, including the UK, you may need to report your condition to the relevant agency (such as the DVLA) or face a fine or other punishment.
12. What are possible alternatives to EYLEA?
Anti-VEGF treatment is a relatively recent development and is considered superior and more effective than older options, such as photodynamic therapy, in the treatment of wet AMD and macular edema.
EYLEA is one of four anti-VEGF drugs on the market, alongside Lucentis (ranibizumab), Beovu (brolucizumab), and Avastin (bevacizumab). Like EYLEA, Lucentis and Beovu are approved by the FDA for treating wet AMD and other eye conditions, while Avastin is approved to treat several cancers.
While Avastin is not approved to treat wet AMD or other eye conditions, it is considered safe and effective and is often used because it is cheaper. However, this may depend on where you live and your insurance coverage. As mentioned in an earlier question, What is the difference between aflibercept and ziv-aflibercept?, ziv-aflibercept (Zaltrap) has been tested to treat eye conditions. However, its safety profile is not as well defined as that of Avastin.
While other types of treatment, including high-dose intravitreal triamcinolone acetonide (ITVA) and atypical protein kinase C (aPKC) inhibitors, have been touted as possible alternatives, anti-VEGF treatment is usually still considered the first-line treatment for wet AMD.
Alternative treatment may be used for macular edema, including steroids, eye drops, and laser treatment, but these are often when the underlying cause is different from those discussed in this article.
You should speak to your doctor about your specific condition and the treatment options available.
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