Medicine overview
Indications of Zaltrap
Zaltrap is a recombinant fusion protein (a "VEGF-trap") administered by intravitreal injection. It is FDA-approved for the following ophthalmic indications:
- Neovascular (wet) age-related macular degeneration (AMD) – established, FDA-approved primary indication.
- Diabetic macular edema (DME) – established, FDA-approved indication.
- Diabetic retinopathy (DR), with or without DME – established, FDA-approved indication.
- Macular edema following retinal vein occlusion (RVO), both central and branch RVO – established, FDA-approved indication.
- Retinopathy of prematurity (ROP) in preterm infants – FDA-approved indication using a lower, weight-adjusted dose.
Zaltrap is not curative; it reduces disease-related vision loss and requires an individualized, ongoing injection schedule determined by a qualified ophthalmologist.
Composition
Each single-dose vial or pre-filled syringe contains Aflibercept 40 mg/mL solution for intravitreal injection, delivering a 2 mg dose in 0.05 mL for standard-strength products. Aflibercept is produced using recombinant DNA technology in a Chinese hamster ovary (CHO) cell expression system.
Description
Zaltrap is a recombinant fusion protein consisting of portions of human VEGF receptors 1 and 2 fused to the Fc portion of human IgG1, formulated as an iso-osmotic solution for intravitreal injection. It acts as a soluble decoy receptor that binds and neutralizes vascular endothelial growth factor-A (VEGF-A) and placental growth factor (PlGF), blocking signaling that drives abnormal retinal blood vessel growth and vascular leakage. Zaltrap is administered only by intravitreal injection performed by a qualified ophthalmologist under sterile conditions; it is not a self-administered medicine.
Therapeutic Class
Zaltrap belongs to the class of anti-vascular endothelial growth factor (anti-VEGF) agents, specifically a VEGF-trap fusion protein used in ophthalmology for retinal vascular disease.
Pharmacology
Mechanism
Aflibercept functions as a soluble decoy receptor that binds VEGF-A, VEGF-B, and placental growth factor (PlGF) with high affinity, preventing these factors from binding to and activating VEGFR-1 and VEGFR-2 on vascular endothelial cells. By neutralizing these growth factors, Aflibercept suppresses neovascularization and reduces vascular permeability in the retina and choroid.
Pharmacokinetics
After intravitreal injection, Aflibercept is slowly absorbed into the systemic circulation; plasma concentrations are low and systemic exposure is minimal at recommended doses. Vitreous half-life is approximately 5–7 days, supporting dosing intervals of 4 to 16 weeks depending on indication and response.
Dosage & Administration of Zaltrap
Zaltrap is administered only as an intravitreal injection (2 mg/0.05 mL per eye) by a qualified ophthalmologist experienced in intravitreal procedures, under strict aseptic technique. Recommended dosing schedules differ by indication:
| Indication | Initial Phase | Maintenance Phase |
|---|---|---|
| Neovascular (wet) AMD | 2 mg every 4 weeks for the first 3 injections | 2 mg every 8 weeks thereafter; some patients may need every-4-week dosing |
| Diabetic Macular Edema (DME) | 2 mg every 4 weeks for the first 5 injections | 2 mg every 8 weeks thereafter |
| Diabetic Retinopathy (DR) | 2 mg every 4 weeks for the first 5 injections | 2 mg every 8 weeks thereafter |
| Macular Edema following RVO | 2 mg every 4 weeks | Continued monthly dosing; interval extension considered based on response |
| Retinopathy of Prematurity (ROP), preterm infants | 0.4 mg (0.01 mL) single dose per eye | Repeat only if disease reactivation is documented, per specialist assessment |
No dose adjustment of Zaltrap is required for renal or hepatic impairment, as systemic exposure after intravitreal use is minimal.
Administration of Zaltrap
Zaltrap must be administered only by intravitreal injection performed by a qualified ophthalmologist in a controlled, aseptic clinical setting. Before each injection, adequate anesthesia and a broad-spectrum topical microbicide are applied to the periocular skin, eyelid, and ocular surface, and the injection is given into the vitreous cavity using a fine-gauge needle under sterile technique. Perfusion of the optic nerve head is checked immediately after injection. Patients receiving Zaltrap must be instructed to report any eye pain, redness, photophobia, blurred or decreased vision, or increased floaters without delay. Zaltrap is not intended for self-administration or administration by non-ophthalmologist personnel.
Interaction of Zaltrap
No formal systemic drug-drug interaction studies have been conducted with Zaltrap, and clinically significant systemic interactions are not expected because systemic exposure after intravitreal administration is minimal. Zaltrap should be used with caution when other intravitreal anti-VEGF agents are used in the same eye, and Zaltrap injections should not be combined with other intraocular procedures unless directed by the treating ophthalmologist. Caution is advised when Zaltrap is used in patients also receiving systemic anti-angiogenic therapy, given the shared class-related risk of arterial thromboembolic events.
Contraindications
Aflibercept is contraindicated in patients with:
- Ocular or periocular infection.
- Active severe intraocular inflammation.
- Known hypersensitivity to Aflibercept or to any component of the formulation.
Side Effects of Zaltrap
The most common adverse reactions associated with Zaltrap injection relate to the eye and the injection procedure itself:
- Conjunctival hemorrhage
- Eye pain
- Cataract
- Vitreous floaters/detachment
- Increased intraocular pressure
- Corneal abrasion
Serious but uncommon reactions include endophthalmitis, retinal detachment, retinal tear, traumatic cataract from the injection, and rarely, arterial thromboembolic events such as stroke or myocardial infarction, recognized as a class effect of intravitreal anti-VEGF agents (see Precautions and Warnings). Patients should seek prompt ophthalmologic evaluation for any sudden change in vision or eye symptoms after an Zaltrap injection.
Pregnancy & Lactation
Zaltrap has anti-VEGF activity that could affect placental and fetal vascular development, even though systemic absorption after intravitreal injection is low. Zaltrap should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus, and only after consultation with a physician. It is not known whether Zaltrap passes into human breast milk; because effects on a nursing infant cannot be excluded, a decision on whether to continue breastfeeding or continue Zaltrap treatment should be made in consultation with a physician, weighing the importance of treatment to the mother. Women of reproductive potential should discuss contraception with their physician before and after Zaltrap treatment.
Precautions & Warnings
Zaltrap must be administered only by a qualified ophthalmologist by intravitreal injection under sterile conditions; it is not intended for patient self-administration.
- Endophthalmitis and retinal detachment: Rare but serious risks of the intravitreal injection procedure. Patients must be instructed to report eye pain, worsening redness, photophobia, blurred or decreased vision, or increased floaters immediately.
- Increased intraocular pressure: Transient elevations in IOP can occur shortly after injection; IOP and optic nerve head perfusion should be monitored.
- Arterial thromboembolic events (ATE): Stroke and myocardial infarction have been reported with intravitreal anti-VEGF agents as a class; use caution in patients with a recent history of these events.
- Ongoing monitoring required: Zaltrap does not cure the underlying retinal disease; regular ophthalmologic follow-up and repeated injections per protocol are needed for sustained benefit.
Overdose Effects of Zaltrap
Overdose with Zaltrap is uncommon since it is administered by a healthcare professional in controlled doses, but accidental administration of a higher volume or more frequent injections has been reported and may increase intraocular pressure or cause other ocular adverse effects. If overdose is suspected, the patient should be monitored closely by an ophthalmologist, intraocular pressure should be measured and managed as needed, and if any systemic symptoms occur, immediate medical attention or contact with emergency services or a poison control center is advised.
Storage Conditions
Store Zaltrap pre-filled syringes or vials refrigerated at 2°C to 8°C (36°F to 46°F). Do not freeze. Protect from light by keeping the syringe/vial in its original carton until ready to use. Unopened, unused Zaltrap may be kept at room temperature (up to 25°C/77°F) for up to 24 hours prior to use. Keep out of reach of children. Zaltrap is for single use only per injection; discard any unused portion.
Use In Special Populations
Renal/Hepatic impairment: No dose adjustment of Zaltrap is required, as systemic exposure after intravitreal administration is minimal, and formal studies in these populations have not been conducted.
Elderly: No overall differences in safety or efficacy have been observed in elderly patients; most patients treated for wet AMD are elderly.
Pediatric use: Zaltrap is approved specifically for retinopathy of prematurity (ROP) at a reduced dose; safety and efficacy for other pediatric retinal indications have not been established (see Pediatric Uses).
Duration Of Treatment
Treatment with Zaltrap is long-term and individualized. After an initial series of monthly injections (frequency depends on indication), the ophthalmologist may extend the interval based on anatomic and visual response, typically up to every 8–16 weeks. Zaltrap treatment is generally continued indefinitely as long as active disease and treatment benefit persist, since the underlying retinal disease is chronic and Zaltrap does not provide a permanent cure.
Drug Classes
Aflibercept is classified as an anti-vascular endothelial growth factor (anti-VEGF) agent / VEGF-trap fusion protein, within the broader group of ophthalmic angiogenesis inhibitors.
Mode Of Action
Aflibercept acts as a soluble decoy receptor: it binds circulating and tissue VEGF-A, VEGF-B, and placental growth factor (PlGF) with high affinity, preventing these ligands from binding to and activating native VEGF receptors (VEGFR-1 and VEGFR-2) on retinal and choroidal vascular endothelial cells. This blocks downstream signaling that drives pathological neovascularization and vascular permeability, reducing macular edema and abnormal vessel growth.
Pregnancy
C
Pediatric Uses
The safety and efficacy of Zaltrap have been established specifically for the treatment of retinopathy of prematurity (ROP) in preterm infants, using a reduced dose of 0.4 mg (0.01 mL) per eye administered by intravitreal injection by an ophthalmologist experienced in treating ROP. Safety and efficacy of Zaltrap for other pediatric retinal conditions (which are rare in children) have not been established, and use in these settings should only be considered by a pediatric ophthalmology specialist when no suitable alternative exists.
Frequently Asked Questions
Q: What is Zaltrap 100 mg/4 ml IV Infusion used for?
A: Zaltrap 100 mg/4 ml IV Infusion is an anti-VEGF injection used by ophthalmologists to treat wet age-related macular degeneration, diabetic macular edema, diabetic retinopathy, macular edema after retinal vein occlusion, and, at a lower dose, retinopathy of prematurity in preterm infants.
Q: How is Zaltrap 100 mg/4 ml IV Infusion given?
A: Zaltrap 100 mg/4 ml IV Infusion is given only as an intravitreal injection directly into the eye by a qualified ophthalmologist under sterile conditions in a clinic or operating room; it is never self-injected at home.
Q: How often will I need Zaltrap 100 mg/4 ml IV Infusion injections?
A: Most patients start with monthly Zaltrap 100 mg/4 ml IV Infusion injections for the first 3 to 5 doses, after which the ophthalmologist may extend the interval to every 8 weeks or longer depending on how the eye responds. Zaltrap 100 mg/4 ml IV Infusion treatment is usually needed on an ongoing basis, as it controls but does not cure the underlying retinal disease.
Q: What warning signs should I report after an Zaltrap 100 mg/4 ml IV Infusion injection?
A: Contact your ophthalmologist immediately if you notice eye pain, worsening redness, sensitivity to light, blurred or decreased vision, or a sudden increase in floaters after an Zaltrap 100 mg/4 ml IV Infusion injection, as these can be signs of rare but serious complications such as endophthalmitis (infection) or retinal detachment.
Q: Is Zaltrap 100 mg/4 ml IV Infusion safe during pregnancy?
A: Zaltrap 100 mg/4 ml IV Infusion should be used during pregnancy only if clearly needed and if the potential benefit justifies the potential risk to the fetus, since Zaltrap 100 mg/4 ml IV Infusion can affect blood vessel growth important for fetal development; always consult your physician before using Zaltrap 100 mg/4 ml IV Infusion if you are pregnant or planning pregnancy.
Q: Who should not receive Zaltrap 100 mg/4 ml IV Infusion?
A: Zaltrap 100 mg/4 ml IV Infusion should not be given to patients with an active infection in or around the eye, active severe inflammation inside the eye, or known hypersensitivity to Zaltrap 100 mg/4 ml IV Infusion or its ingredients.
Disclaimer
The information provided is accurate to the best of our knowledge, but it does not replace professional medical advice. We cannot guarantee its completeness or accuracy, and the absence of specific information about a drug should not be taken as an endorsement. We are not responsible for any consequences arising from this information, so please consult a healthcare professional for any concerns or questions.
