EYLEA is a brand name for a medication called aflibercept. It is primarily used as an injection to treat various eye conditions.
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.
Aflibercept acts as a soluble decoy receptor that binds VEGF-A and PlGF, and thereby can inhibit the binding and activation of these cognate VEGF receptors.
Indication:
- Wet age-related macular degeneration (AMD): This is the most common use of EYLEA. It helps slow vision loss caused by abnormal blood vessel growth and leakage in the eye.
- Diabetic macular edema (DME): This is swelling of the macula due to diabetes, and EYLEA can help improve vision and reduce swelling.
- Retinal vein occlusion (RVO): Blockage of blood vessels in the retina can cause vision loss, and EYLEA can help restore vision and reduce swelling.
- Diabetic retinopathy (DR): EYLEA may be used in some cases of advanced DR to reduce abnormal blood vessel growth and prevent vision loss.
- Retinopathy of prematurity (ROP): In premature babies, EYLEA can help abnormal blood vessels in the eye develop normally, reducing the risk of vision problems.
Dosage form and Composition:
- EYLEA is available as a sterile solution for injection into the eye (intravitreal injection).
- EYLEA is a sterile, clear, and colorless to pale yellow solution. EYLEA does not contain anti-microbial preservative and is supplied as a sterile, aqueous solution for intravitreal injection in a single-dose pre-filled glass syringe or a single-dose glass vial designed to deliver 0.05 mL (50 microliters) of solution containing 2 mg of aflibercept in polysorbate 20 (0.015 mg), sodium chloride (0.117 mg), sodium phosphate monobasic monohydrate (0.055 mg), sodium phosphate dibasic heptahydrate (0.027 mg), sucrose (2.5 mg) and water for injection with a pH of 6.2.
EYLEA is a clear, colorless to pale yellow solution available as:
- Injection: 2 mg (0.05 mL of a 40 mg/mL solution) in a single-dose pre-filled glass syringe
- Injection: 2 mg (0.05 mL of a 40 mg/mL solution) in a single-dose glass vial.
Dose:
- The dose and dosing schedule vary depending on the specific condition being treated and the individual patient's needs.
- Typically, for wet AMD and DME, the initial dose is 2mg every 4 weeks for the first 5 injections, followed by 2mg every 8 weeks. Adjustments may be made based on individual response.
Route of administration:
- EYLEA is administered as an intravitreal injection, directly into the vitreous humor (jelly-like substance) in the eye. This is done by an ophthalmologist in a clinical setting.
Effectiveness compared to its peer group:
- EYLEA is considered one of the most effective medications for wet AMD and DME, comparable to other anti-VEGF drugs like Lucentis and Avastin.
- Studies have shown similar effectiveness in terms of improving vision and reducing swelling.
- The choice of medication may depend on factors such as individual response, cost, and potential side effects.
Adverse events:
- Like any medication, EYLEA can have side effects. Some common side effects include:
- Eye pain, redness, or irritation
- Increased floaters
- Bleeding in the eye
- Eye infection (endophthalmitis)
- Increased blood pressure
- Nosebleeds
- More serious side effects are rare but can occur, such as stroke, heart attack, or allergic reaction.
- It is important to discuss the potential risks and benefits of EYLEA with your doctor before starting treatment.
Recent News - Lawsuits
On November 29, 2023, Regeneron Pharmaceuticals, Inc. filed a Compliant against Formycon AG (“Formycon”) in the U.S. District Court for the Northern District of West Virginia, alleging infringement of 39 patents under the BPCIA based on Formycon’s submission of an aBLA for FYB203, a proposed biosimilar of EYLEA (aflibercept). According to the news, this was the fourth infringement suit under the BPCIA concerning a proposed biosimilar of EYLEA, after Regeneron sued Mylan (August 2, 2022), Celltrion (November 8, 2023), and Samsung Bioepis (November 22, 2023).
Regeneron states that the use of Formycon's FYB203 will infringe multiple related to the methods of adminstering aflibercept, stable formulations of aflibercept, and its manufacturing process, totally 3 groups. And here are the 3 groups of patents:
8 method of treatment patents: U.S. Patent Nos. 9,254,338; 10,130,681; 10,828,345; 10,888,601; 11,253,572; 11,559,564; 11,707,506; and 11,769,597.
4 formulation patents: U.S. Patent Nos. 10,464,992; 11,066,458; 11,084,865; and 11,732,024.
27 manufacturing process patents: U.S. Patent Nos. 7,070,959; 7,771,997; 9,222,106; 9,562,238; 9,816,110; 9,932,605; 10,415,055; 10,669,594; 10,927,342; 11,053,280; 11,104,715; 11,174,283; 11,268,109; 11,299,532; 11,306,135; 11,312,936; 11,332,771; 11,472,861; 11,485,770; 11,535,663; 11,542,317; 11,548,932; 11,549,154; 11,555,176; 11,680,930; 11,753,459 and 11,788,102.
Here is the list of Purple Book Patents for Eylea (aflibercept)
Reference:
Product Insert,
Kristin M. Beale, Regeneron sues Formycon AG for proposed biosimilar of EYLEA in West Virginia District Court, Bio Molecule Watch, December 11, 2023. Assessed on Feb 06, 2024.
