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SENSORY ORGANS › OPHTHALMOLOGICALS › OCULAR VASCULAR DISORDER AGENTS › Antineovascularisation agents
aflibercept
S01LA05
Forms & Strengths
- Intravitreal injection: 2 mg/0.05 mL (40 mg/mL) in a single-dose vial
- Intravitreal injection: 2 mg/0.05 mL in a pre-filled syringe
- Intravitreal injection (High Dose): 8 mg/0.070 mL (114.3 mg/mL) in a single-dose vial
Adult Dosing
- Neovascular (wet) AMD (2 mg): 2 mg (0.05 mL) monthly for the first 3 months, then 2 mg every 2 months (8 weeks)
- Neovascular (wet) AMD (8 mg): 8 mg (0.07 mL) every 4 weeks for the first 3 doses, then every 8 to 16 weeks
- Macular Edema following RVO: 2 mg (0.05 mL) monthly
- Diabetic Macular Edema (2 mg): 2 mg (0.05 mL) monthly for the first 5 months, then 2 mg every 2 months (8 weeks)
- Diabetic Macular Edema (8 mg): 8 mg (0.07 mL) every 4 weeks for the first 5 doses, then every 8 to 16 weeks
- Diabetic Retinopathy: 2 mg (0.05 mL) monthly for the first 5 months, then 2 mg every 2 months (8 weeks)
Pediatric Dosing
- Safety and efficacy have not been established in pediatric patients
Indications
- Neovascular (wet) Age-Related Macular Degeneration (AMD)
- Macular Edema following Retinal Vein Occlusion (RVO)
- Diabetic Macular Edema (DME)
- Diabetic Retinopathy (DR) in patients with DME
- Retinopathy of Prematurity (ROP) - select formulations/regions
Mechanism of Action
- Recombinant fusion protein consisting of portions of human VEGF receptors 1 and 2 extracellular domains fused to the Fc portion of human IgG1
- Acts as a soluble decoy receptor that binds VEGF-A, VEGF-B, and placental growth factor (PlGF)
- Inhibits the binding and activation of cognate VEGF receptors, thereby suppressing endothelial cell proliferation, vascular permeability, and neovascularization
Contraindications
- Ocular or periocular infections
- Active severe intraocular inflammation
- Known hypersensitivity to aflibercept or any of the excipients
Adverse Reactions
- Conjunctival hemorrhage
- Eye pain
- Cataract
- Vitreous detachment
- Vitreous floaters
- Increased intraocular pressure
- Endophthalmitis (rare)
- Retinal detachment (rare)
- Arterial thromboembolic events (systemic risk)
Drug Interactions
- Formal clinical drug interaction studies have not been performed with intravitreal administration
- Potential additive systemic effects when combined with other inhibitors of VEGF
Curated Content: Needs Vetting Before Put to Clinical Use