MACUGEN (pegaptanib) the treatment of neovascular (wet) age-related macular degeneration

Pegaptanib is a selective vascular endothelial growth factor (VEGF) antagonist. VEGF is a secreted protein that selectively binds and activates its receptors located primarily on the surface of vascular endothelial cells. VEGF induces angiogenesis, and increases vascular permeability and inflammation, all of which are thought to contribute to the progression of the neovascular (wet) form of age-related macular degeneration (AMD), a leading cause of blindness. VEGF has been implicated in blood retinal barrier breakdown and pathological ocular neovascularization. 

Pegaptanib is an aptamer, a pegylated modified oligonucleotide, which adopts a threedimensional conformation that enables it to bind to extracellular VEGF. Under in vitro testing conditions, pegaptanib binds to the major pathological VEGF isoform, extracellular VEGF165, thereby inhibiting VEGF165 binding to its VEGF receptors. The inhibition of VEGF164, the rodent counterpart of human VEGF165, was effective at suppressing pathological neovascularization.

INDICATIONS AND USAGE

Macugen is indicated for the treatment of neovascular (wet) age-related macular degeneration

DOSAGE AND ADMINISTRATION

FOR OPHTHALMIC INTRAVITREAL INJECTION ONLY- Macugen 0.3 mg should be administered once every six weeks by intravitreous injection into the eye to be treated 

DOSAGE FORMS AND STRENGTHS

0.3 mg/90 µL solution in a single-use syringe for intravitreal injection

CONTRAINDICATIONS

• Ocular or periocular infections
• Hypersensitivity 

WARNINGS AND PRECAUTIONS 

• Endophthalmitis may occur following intravitreous injections. Proper aseptic injection technique should always be utilized when administering Macugen. Patients should be monitored during the week following the injection 
• Increases in intraocular pressure have been seen within 30 minutes of injection of Macugen.
• Rare cases of anaphylaxis/anaphylactoid reactions, including angioedema, have been reported in the postmarketing experience.

ADVERSE REACTIONS

Most common adverse reactions (reported in 10-40% of patients treated with Macugen for up to two years) are anterior chamber inflammation, blurred vision, cataract, conjunctival hemorrhage, corneal edema, eye discharge, eye irritation, eye pain, hypertension, increased intraocular pressure (IOP), ocular discomfort, punctate keratitis, reduced visual acuity, visual disturbance, vitreous floaters, and vitreous opacities