Afqlir: Uses, Dosage & Side Effects

What Is Afqlir and What Is It Used For?

Afqlir contains the active substance aflibercept, a recombinant fusion protein produced in Chinese hamster ovary (CHO) cells using recombinant DNA technology. Structurally, aflibercept is composed of portions of the extracellular domains of human vascular endothelial growth factor receptor 1 (VEGFR-1) and vascular endothelial growth factor receptor 2 (VEGFR-2), which are fused to the Fc portion of human immunoglobulin G1 (IgG1). This unique molecular design gives aflibercept its characteristic ability to act as a “VEGF trap” – a soluble decoy receptor that binds to VEGF-A, VEGF-B, and placental growth factor (PlGF) with very high affinity, effectively neutralizing these growth factors before they can activate their natural receptors on blood vessel cells.

Vascular endothelial growth factor (VEGF) is a key signaling protein that stimulates the growth of new blood vessels (angiogenesis) and increases vascular permeability (the leakiness of blood vessel walls). Under normal physiological conditions, VEGF plays important roles in wound healing and tissue repair. However, in several retinal diseases, the overproduction of VEGF leads to pathological consequences: the growth of abnormal, fragile new blood vessels (choroidal neovascularization) that can leak fluid and blood beneath or within the retina, causing swelling (macular edema), scarring, and ultimately irreversible damage to the photoreceptor cells responsible for central vision. By binding VEGF-A with higher affinity than its natural receptors, aflibercept prevents the activation of VEGF signaling pathways, thereby reducing neovascularization, decreasing vascular permeability, and limiting retinal damage.

In addition to binding VEGF-A (the primary driver of ocular neovascularization), aflibercept also binds VEGF-B and placental growth factor (PlGF). PlGF has been shown to act synergistically with VEGF-A to promote pathological angiogenesis and inflammation, and its elevated levels have been detected in the vitreous fluid of patients with diabetic macular edema and wet AMD. The dual blockade of VEGF-A and PlGF may provide additional therapeutic benefit beyond VEGF-A inhibition alone, particularly in inflammatory components of retinal disease.

Afqlir is a biosimilar medicine, meaning it has been developed to be highly similar to an already authorized biological reference medicine (Eylea, manufactured by Bayer). Biosimilar medicines undergo an extensive regulatory pathway that includes comprehensive analytical characterization, preclinical (non-clinical) studies, and clinical trials to demonstrate that there are no clinically meaningful differences from the reference product in terms of quality, biological activity, safety, and efficacy. The biosimilar development pathway is scientifically rigorous and is based on the principle that extensive analytical comparability, combined with targeted clinical studies, can establish similarity to a reference product whose safety and efficacy have been established through years of clinical use.

Approved Indications

Afqlir is indicated for the treatment of the following conditions in adults:

• Neovascular (wet) age-related macular degeneration (AMD): The most common cause of severe, irreversible vision loss in adults over 50 in the developed world. In wet AMD, abnormal blood vessels grow beneath the retina (choroidal neovascularization), leaking fluid and blood that damage the macula – the central part of the retina responsible for sharp, detailed vision. Aflibercept has been shown in the VIEW 1 and VIEW 2 clinical trials to produce visual acuity gains comparable to ranibizumab, with the added convenience of less frequent dosing during the maintenance phase.
• Visual impairment due to diabetic macular edema (DME): A complication of diabetes mellitus in which chronically elevated blood glucose levels damage retinal blood vessels, leading to leakage of fluid into the macula. DME is the leading cause of vision loss in working-age adults with diabetes. The VIVID and VISTA trials demonstrated that aflibercept significantly improved visual acuity compared with laser photocoagulation in patients with DME, with benefits sustained over multiple years of treatment.
• Macular edema secondary to retinal vein occlusion (RVO): Both branch retinal vein occlusion (BRVO) and central retinal vein occlusion (CRVO) can cause sudden, painless vision loss when a retinal vein becomes blocked, leading to fluid accumulation in the macula. The COPERNICUS and GALILEO trials (for CRVO) and the VIBRANT trial (for BRVO) demonstrated rapid and sustained visual improvement with aflibercept treatment.
• Visual impairment due to myopic choroidal neovascularization (myopic CNV): In highly myopic individuals (pathologic myopia), abnormal blood vessels may develop beneath the retina, causing fluid leakage and central vision loss. The MYRROR trial demonstrated significant visual improvement with aflibercept in patients with myopic CNV.

What Should You Know Before Taking Afqlir?

Contraindications

Afqlir must not be used in the following situations. Your ophthalmologist will carefully assess these factors before administering each injection:

• Hypersensitivity: Known hypersensitivity (allergy) to aflibercept or to any of the excipients in the formulation. Signs of hypersensitivity may include rash, itching, urticaria (hives), or in rare cases, anaphylaxis. If you have experienced an allergic reaction to any anti-VEGF medication, inform your doctor.
• Active or suspected ocular or periocular infection: The injection must not be given if there is an active infection in or around the eye, as intravitreal injection during an active infection could significantly worsen the infection and risk endophthalmitis (a sight-threatening infection inside the eye).
• Active severe intraocular inflammation (uveitis): Injection should not be performed during episodes of active severe inflammation within the eye, as this could exacerbate the inflammatory process and lead to complications.

Warnings and Precautions

Before and during treatment with Afqlir, the following warnings and precautions should be considered:

• Endophthalmitis and retinal detachment: As with any intravitreal injection procedure, there is a risk of endophthalmitis (incidence approximately 0.02–0.05% per injection) and rhegmatogenous retinal detachment. Strict aseptic injection technique is essential. Patients should be instructed to report any symptoms suggestive of endophthalmitis or retinal detachment without delay.
• Increased intraocular pressure (IOP): Transient increases in IOP have been observed within 60 minutes of intravitreal injection. Sustained IOP increases have also been reported with repeated dosing. IOP should be monitored and managed appropriately, particularly in patients with glaucoma. Treatment should not be given if IOP is 30 mmHg or higher.
• Arterial thromboembolic events: There is a theoretical risk of arterial thromboembolic events (such as stroke or myocardial infarction) associated with systemic VEGF inhibition. Although systemic exposure after intravitreal injection is very low, the risk should be considered, particularly in patients with a history of stroke, transient ischemic attack, or myocardial infarction. Clinical trial data have not shown a significantly increased risk, but caution is warranted.
• Immunogenicity: As a protein therapeutic, aflibercept has the potential to induce an immune response. Anti-drug antibodies have been detected in a small proportion of patients, though these have generally not been associated with clinical consequences such as reduced efficacy or hypersensitivity reactions. If you notice that the treatment seems to be becoming less effective, inform your ophthalmologist.
• Bilateral treatment: The safety and efficacy of concurrent bilateral treatment (injecting both eyes on the same day) have not been established. If both eyes require treatment, separate injection sessions should be considered to reduce the risk of bilateral complications.

Pregnancy and Breastfeeding

Afqlir should not be used during pregnancy unless the potential benefit to the mother outweighs the potential risk to the fetus. Aflibercept has been shown to cause embryo-fetal toxicity in animal studies, including external, visceral, and skeletal malformations, when administered at systemic exposures significantly higher than those achieved with intravitreal injection. Although systemic exposure following intravitreal injection is very low, the inhibition of VEGF could theoretically affect embryo-fetal development.

Women of childbearing potential should use effective contraception during treatment with Afqlir and for at least 3 months after the last intravitreal injection. If pregnancy is discovered during treatment, the potential risks should be discussed with the treating physician and treatment continuation should be carefully considered.

It is not known whether aflibercept is excreted in human breast milk. A risk to the breastfed infant cannot be excluded. Breastfeeding is not recommended during treatment with Afqlir. A decision must be made whether to discontinue breastfeeding or to discontinue treatment, taking into account the benefit of breastfeeding for the child and the benefit of therapy for the woman.

How Does Afqlir Interact with Other Drugs?

Unlike orally or intravenously administered medications that achieve high systemic concentrations, aflibercept is injected directly into the vitreous cavity of the eye. The resulting systemic exposure is extremely low – free aflibercept plasma concentrations after intravitreal injection are typically undetectable or well below the levels required to inhibit systemic VEGF by 50%. Because of this minimal systemic exposure, traditional pharmacokinetic drug interactions mediated through hepatic cytochrome P450 (CYP) enzymes, drug transporters, or plasma protein binding are not expected with Afqlir.

However, there are several clinical scenarios where the interaction between aflibercept and other therapeutic agents warrants careful consideration by the treating ophthalmologist:

Major Interactions

The most clinically relevant interaction consideration is the concurrent use of Afqlir with other anti-VEGF agents, whether administered intravitreally or systemically. Simultaneous use of two intravitreal anti-VEGF agents has not been shown to provide superior efficacy and may increase the risk of adverse events, including heightened intraocular inflammation and elevated intraocular pressure. Patients receiving systemic anti-VEGF therapy (such as bevacizumab for cancer treatment) who also require intravitreal anti-VEGF injections should be closely monitored for potential additive effects, including arterial thromboembolic events and hypertension, although the systemic contribution from intravitreal dosing is minimal.

Minor Interactions

Patients taking anticoagulant or antiplatelet medications may have a slightly increased risk of bleeding complications at the injection site, most commonly subconjunctival hemorrhage. This is generally self-limiting and does not require discontinuation of these medications. Current ophthalmology guidelines recommend that anticoagulants and antiplatelet agents generally should not be discontinued before intravitreal injections, as the risk of systemic thromboembolic events from stopping these medications typically outweighs the minor risk of localized ocular hemorrhage. Your ophthalmologist and prescribing physician should coordinate care if you have questions about your anticoagulation regimen.

What Is the Correct Dosage of Afqlir?

Afqlir must be administered by a qualified ophthalmologist experienced in performing intravitreal injections under aseptic conditions. The recommended dose for all approved indications is 2 mg aflibercept, corresponding to an injection volume of 0.05 mL from the 40 mg/mL solution. The injection is delivered directly into the vitreous cavity of the affected eye using a 30-gauge injection needle.

Adults

For adults with neovascular (wet) AMD, the treatment is initiated with three consecutive monthly injections (loading phase), followed by one injection every 2 months during the first year. After the first year, the injection interval may be extended to every 3 months (treat-and-extend approach) based on the patient’s visual acuity and retinal findings on optical coherence tomography (OCT). The maximum recommended interval between doses is 3 months for wet AMD.

For diabetic macular edema (DME), treatment begins with five consecutive monthly injections (a longer loading phase reflecting the pathophysiology of diabetic retinal disease), followed by one injection every 2 months. After the first 12 months, a treat-and-extend approach may be adopted, where injection intervals are progressively extended by 2-week increments as long as the patient’s visual and anatomic status remains stable.

For retinal vein occlusion (both BRVO and CRVO), treatment is initiated with monthly injections. For BRVO, after 3 initial monthly injections, the interval may be gradually extended. For CRVO, monthly injections are continued until maximum visual improvement is achieved (typically assessed by three consecutive monthly stable acuity measurements), after which the injection interval may be gradually extended.

Children

Afqlir is not recommended for use in children and adolescents under 18 years of age. The safety and efficacy of aflibercept in this population have not been established. The conditions for which aflibercept is indicated (wet AMD, DME, RVO, myopic CNV) are overwhelmingly diseases of adulthood, particularly middle-aged and elderly populations.

Elderly

No dose adjustment is required for elderly patients. The majority of patients treated with aflibercept in clinical trials were over 65 years of age, and the efficacy and safety profile was consistent across age groups. However, elderly patients may have a higher prevalence of comorbidities (such as cardiovascular disease, diabetes, and glaucoma) that require careful monitoring during treatment.

Missed Dose

If a scheduled injection is missed, the appointment should be rescheduled as soon as possible. The treatment should then be continued at the regular intervals previously established. Missing a dose may lead to recurrence of disease activity (fluid accumulation, neovascular growth), which could result in a decline in visual acuity. Patients should be advised about the importance of adhering to their injection schedule and attending all monitoring appointments.

Overdose

Overdose with intravitreal injection is unlikely given that the treatment is administered by a healthcare professional in a clinical setting using a pre-filled syringe or single-use vial designed to deliver a precise volume. If an accidental overdose occurs (injection of more than the recommended 0.05 mL volume), the elevated intraocular pressure should be closely monitored and managed as necessary. The eye should be examined for signs of damage, and the patient should be closely followed in the days after the overdose. There is no specific antidote for aflibercept overdose.

What Are the Side Effects of Afqlir?

As with all medicines, Afqlir can cause side effects, although not everybody gets them. The side effects reported with aflibercept (both the reference product and biosimilars) are well characterized from extensive clinical trial data involving thousands of patients, as well as post-marketing surveillance data collected over more than a decade of clinical use. The majority of adverse reactions are related to the intravitreal injection procedure itself rather than to the pharmacological effects of the drug.

The following side effects are categorized by frequency according to the convention used by the European Medicines Agency (EMA):

The vast majority of side effects associated with aflibercept treatment are mild to moderate in severity and resolve spontaneously without requiring medical intervention. Conjunctival hemorrhage, the most frequently reported adverse event, is typically painless and resolves within 1–2 weeks. Transient increases in intraocular pressure usually normalize within minutes to hours after the injection. Vitreous floaters may persist for days to weeks but gradually diminish over time.

The most clinically significant adverse events are endophthalmitis and retinal detachment. Endophthalmitis is a medical emergency characterized by severe eye pain, progressive vision loss, redness, and often a visible collection of inflammatory cells (hypopyon) in the anterior chamber. If suspected, endophthalmitis requires immediate referral to an ophthalmologist for urgent treatment with intravitreal antibiotics. Retinal detachment may present as a sudden onset of flashing lights, a shower of new floaters, or a curtain-like shadow across the visual field; it also requires urgent ophthalmic assessment and potential surgical intervention.

How Should You Store Afqlir?

Proper storage of Afqlir is essential to maintain the integrity and efficacy of the medication. As a biological medicine (recombinant fusion protein), aflibercept is sensitive to temperature extremes, light exposure, and physical agitation, which can affect the protein structure and potentially reduce its therapeutic activity or increase immunogenicity.

• Refrigerated storage: Store in a refrigerator at 2–8°C (36–46°F). Do not freeze. If the product has been accidentally frozen, it must not be used.
• Light protection: Keep the vial or pre-filled syringe in the original carton to protect from light until the time of use.
• Room temperature: The unopened product may be stored at room temperature (below 25°C / 77°F) for up to 24 hours before use. Once removed from refrigeration, do not return to the refrigerator.
• After preparation: Once the vial has been punctured or the syringe has been prepared for injection, the product should be used immediately. Do not store any unused portion for later use, as preservative-free formulations do not contain antimicrobial agents.
• Visual inspection: Before use, the solution should be visually inspected for particles and discoloration. Afqlir should appear as a clear, colorless to pale yellow solution. Do not use if the solution is cloudy, contains visible particles, or shows discoloration.
• Shelf life: Do not use Afqlir after the expiry date printed on the carton and vial label. The expiry date refers to the last day of that month.

As Afqlir is administered in a clinical setting by a healthcare professional, patients themselves are generally not responsible for storing the medication. However, understanding these requirements can help patients appreciate why their ophthalmologist’s clinic follows specific protocols for medication handling and why appointments should not be significantly delayed once the medication has been prepared.

What Does Afqlir Contain?

Understanding the composition of your medication is important, particularly if you have known allergies or sensitivities to specific pharmaceutical ingredients. Below is a detailed breakdown of what Afqlir contains.

Active Ingredient

The active substance is aflibercept, a recombinant fusion protein produced in Chinese hamster ovary (CHO) cells. Each vial contains aflibercept at a concentration of 40 mg/mL. The recommended single dose of 2 mg is contained in an injection volume of 0.05 mL. Aflibercept is a glycoprotein dimer with a molecular weight of approximately 115 kilodaltons (kDa), consisting of portions of the extracellular domains of human VEGFR-1 and VEGFR-2 fused to the Fc region of human IgG1.

Inactive Ingredients (Excipients)

Appearance and Pack Sizes

Afqlir is supplied as a clear, colorless to pale yellow solution for injection in a single-use glass vial. Each vial contains an overfill to allow extraction of the nominal 0.05 mL dose using the 30-gauge injection needle provided. The vial should be inspected visually before use – do not use if the solution is cloudy, contains particles, or has changed color. Afqlir is available in packs of 1 vial. Not all pack sizes may be marketed in every country.

Marketing Authorization Holder and Manufacturer

Afqlir has been authorized as a biosimilar medicine in the European Union. The marketing authorization was granted based on a comprehensive comparability program demonstrating biosimilarity to the reference product Eylea (aflibercept). Patients and healthcare professionals should always refer to the most current product information approved by their national regulatory authority for the most up-to-date prescribing information.