Aflibercept: Uses, Dosage, Side Effects, and More

Introduction to Aflibercept

Aflibercept is a medication known for its role in treating various eye conditions and certain types of cancer. Available under brand names such as Eylea for eye conditions and Zaltrap for cancer therapy, aflibercept is designed to inhibit the activity of vascular endothelial growth factor (VEGF). By blocking VEGF, aflibercept prevents abnormal blood vessel growth, which is crucial in managing eye diseases and certain types of cancer. This guide offers a detailed overview of aflibercept, its uses, dosage recommendations, potential side effects, interactions with other medications, and frequently asked questions.

What is Aflibercept?

Aflibercept is a fusion protein that targets and binds to VEGF-A, VEGF-B, and placental growth factor (PlGF). VEGF is a protein that promotes the formation of abnormal blood vessels, leading to disease progression in eye conditions and some cancers. By blocking VEGF, aflibercept helps slow or halt the growth of abnormal blood vessels, reducing swelling and inflammation. Aflibercept’s ability to inhibit blood vessel growth makes it valuable in treating various conditions, particularly in ophthalmology and oncology.

Uses of Aflibercept

1. Eye Conditions

• Neovascular (Wet) Age-Related Macular Degeneration (AMD): Aflibercept is commonly used to treat wet AMD, where abnormal blood vessels grow beneath the retina, causing vision loss.
• Diabetic Macular Edema (DME): In patients with diabetes, aflibercept helps reduce swelling in the macula, improving vision.
• Macular Edema Following Retinal Vein Occlusion (RVO): Aflibercept is used to manage swelling in the retina following blockage of the retinal vein.
• Diabetic Retinopathy (DR): Aflibercept is also approved to treat diabetic retinopathy, a diabetes complication that can lead to blindness if left untreated.

2. Cancer Treatment

• Metastatic Colorectal Cancer: Aflibercept, under the brand name Zaltrap, is used in combination with other chemotherapies to treat metastatic colorectal cancer. It works by blocking the blood supply to tumors, slowing their growth.

Dosage and Administration

Aflibercept is administered either as an intravitreal injection (directly into the eye) for eye conditions or as an intravenous infusion for cancer treatment. The dosage and frequency depend on the specific condition being treated.

1. Dosage for Eye Conditions (Eylea):

• Wet AMD: The initial dose is 2 mg (0.05 mL) injected once a month for three months, followed by one injection every two months. Some patients may require more frequent dosing.
• Diabetic Macular Edema (DME) and Diabetic Retinopathy (DR): The initial dosage is 2 mg once a month for five injections, followed by injections every two months.
• Macular Edema Following RVO: The recommended dose is 2 mg once a month.

2. Dosage for Cancer Treatment (Zaltrap):

• For metastatic colorectal cancer, aflibercept is administered as an intravenous infusion at a dose of 4 mg/kg over one hour every two weeks, in combination with FOLFIRI (folinic acid, 5-fluorouracil, and irinotecan).

3. Administration Instructions:

• For Eye Conditions: A healthcare provider administers the intravitreal injection in a clinical setting. Local anesthesia and antiseptic eye drops are applied to minimize discomfort and reduce infection risk.
• For Cancer Treatment: Aflibercept is given as an IV infusion under close medical supervision to monitor for any immediate adverse reactions.

Side Effects of Aflibercept

While aflibercept is generally well tolerated, it may cause side effects that vary depending on the treatment area. Patients should be aware of potential side effects and communicate with their healthcare provider if they experience any unusual symptoms.

Common Side Effects

1. For Eye Conditions (Eylea):

• Eye Pain: Some patients may experience mild to moderate pain in the treated eye.
• Blurred Vision: Blurred vision is common and usually temporary after the injection.
• Increased Eye Pressure: Increased intraocular pressure may occur shortly after injection, and regular eye exams are necessary.
• Conjunctival Hemorrhage: Small bleeds in the white of the eye can occur but usually resolve on their own.

2. For Cancer Treatment (Zaltrap):

• Fatigue and Weakness: Many patients report feeling tired or weak.
• Diarrhe Gastrointestinal side effects like diarrhea are common and may require supportive care.
• Stomatitis (Mouth Sores): Painful mouth sores can develop, especially when combined with chemotherapy.
• Hypertension (High Blood Pressure): Elevated blood pressure may occur and should be managed with appropriate medications.

Serious Side Effects

1. Endophthalmitis: This serious eye infection can occur following intravitreal injection and requires immediate medical attention.

2. Retinal Detachment: Although rare, retinal detachment is a serious complication of aflibercept eye injections.

3. Gastrointestinal Perforation (Zaltrap): In cancer patients, there is a risk of gastrointestinal perforation, which can be life-threatening and requires urgent care.

4. Thromboembolic Events: Blood clots, including stroke and heart attack, are potential risks in cancer treatment.

Interaction with Other Medications

Aflibercept’s interaction profile varies depending on the form and specific usage. Patients should always inform their healthcare providers of all medications, supplements, and herbs they are using.

1. Anti-VEGF Agents: Using aflibercept with other anti-VEGF drugs may increase the risk of serious side effects, including blood clots.

2. Blood Pressure Medications: Aflibercept may elevate blood pressure, so patients on antihypertensive medications should have their blood pressure monitored closely.

3. Chemotherapy Agents: When used for cancer, aflibercept is often combined with other chemotherapy drugs, which may increase the risk of adverse reactions. Monitoring by a healthcare provider is necessary.

4. Anticoagulants and Antiplatelets: For patients receiving Zaltrap, the risk of bleeding may increase with anticoagulant drugs, such as warfarin and aspirin, which require close monitoring.

Benefits of Aflibercept

Aflibercept offers several significant benefits, especially for patients with serious eye conditions and advanced cancer. Here are some of its key advantages:

1. Preservation of Vision: Aflibercept has been shown to slow or halt the progression of diseases like AMD and DME, helping preserve and improve vision.

2. Improved Quality of Life for Cancer Patients: By inhibiting blood supply to tumors, aflibercept can slow cancer progression, providing more time and potentially improving the quality of life for patients with metastatic colorectal cancer.

3. Convenient Dosing Schedule for Eye Conditions: Unlike other anti-VEGF treatments, aflibercept’s dosing schedule often requires fewer injections over time, reducing the treatment burden.

4. Targeted Mechanism of Action: As a targeted therapy, aflibercept is designed to act on specific pathways, which may lead to more effective outcomes with potentially fewer systemic side effects.

Frequently Asked Questions (FAQs)

1. What conditions does aflibercept treat?

Aflibercept is used to treat eye diseases such as wet AMD, diabetic macular edema, diabetic retinopathy, and macular edema due to RVO. It is also used to treat metastatic colorectal cancer in combination with chemotherapy.

2. How is aflibercept administered?

For eye conditions, aflibercept is given as an intravitreal injection directly into the eye. For cancer treatment, it is administered as an intravenous infusion.

3. How often do I need aflibercept injections for eye conditions?

The frequency varies based on the condition, but typically, injections are given monthly for the first few doses, followed by one injection every two months or as needed.

4. What are the most common side effects of aflibercept?

Common side effects for eye treatments include eye pain, increased eye pressure, and blurred vision. For cancer treatments, common side effects include fatigue, high blood pressure, and diarrhea.

5. Is aflibercept safe during pregnancy?

Aflibercept is not recommended during pregnancy due to potential risks to the fetus. Women who are pregnant or planning to become pregnant should discuss this with their healthcare provider.

6. Can aflibercept cure macular degeneration?

Aflibercept does not cure macular degeneration. However, it can slow the progression of the disease and help preserve vision.

7. Can I drive after receiving an aflibercept eye injection?

Some patients may experience blurred vision after the injection, so it’s advised to wait until vision clears before driving.

8. What precautions should I take while on aflibercept for cancer?

Patients should monitor for signs of bleeding, avoid using blood-thinning medications unless approved by their healthcare provider, and attend all follow-up appointments for monitoring.

9. Can aflibercept interact with other cancer medications?

Yes, aflibercept may interact with other chemotherapy drugs, increasing the risk of side effects. It is essential to use aflibercept in combination with other treatments only

under close medical supervision.

10. Is aflibercept covered by insurance?

Coverage varies based on the insurance provider and the condition being treated. Patients should verify coverage with their insurance company and explore assistance programs if needed.

Brand Names of Aflibercept

Aflibercept is marketed under the following brand names:

• Eyle For ophthalmic conditions such as AMD, DME, DR, and RVO.
• Zaltrap: For use in combination with chemotherapy for metastatic colorectal cancer.

Conclusion

Aflibercept is a versatile treatment option for various serious conditions, including certain eye diseases and advanced colorectal cancer. Its targeted inhibition of VEGF helps preserve vision, reduce cancer progression, and improve the quality of life for many patients. While aflibercept can provide substantial benefits, it is essential for patients to be aware of potential side effects and interactions, adhering closely to medical guidance for safe and effective use.