Pegaptanib Brand Name– Macugen
What is Pegaptanib
Pegaptanib is an aptamer, a pegylated modified oligonucleotide, that is a selective vascular endothelial growth factor (VEGF) antagonist, a type of signal-transduction inhibitor (STI) and angiogenesis inhibitor.
The agent is a novel intravitreal injection for age-related macular degeneration (AMD), a leading form of blindness.
The drug works by targeting a very specific VEGF isoform involved in the disease process of AMD, known as VEGF-165.
The two pivotal, randomized, double blinded, international clinical trials enrolled patients (n= 1200 total; 892 receiving the drug, 298 receiving placebo) with neovascular AMD including classic, occult, and mixed lesions of up to 12 disc areas; baseline visual acuity in the study eyes ranged from 20/40 and 20/320.
The primary efficacy endpoint was the percent of patients losing < 15 letters of visual acuity from baseline up to the first year assessment.
Pegaptanib treatment met the endpoints for the studies at 1 year.
Verteporfin photodynamic therapy (PDT) was permitted at investigator discretion in those with predominantly classic lesions; more placebo treated patients received PDT than pegaptanib treated patients.
Pegaptanib treated patients and those receiving placebo continued to experience vision loss; however, the rate of vision decline in the pegaptanib treated group was rated slower than that of patients receiving placebo in the first year of use.
Pegaptanib was less effective in the second year of treatment; patients who discontinue therapy experience loss of vision at a similar rate as placebo therapy. It should be noted that antiangiogenic drugs, like pegaptanib, do not restore vision in cases where the photoreceptors are already damaged and degenerated.
The role of agents like pegaptanib is to maintain current vision status or to slow the progression of vision loss.
Investigational uses of pegaptanib include the treatment of diabetic macular edema, Von Hippel-Lindau Disease (benign central nervous system CNS tumors which include angiomas), and retinal vein occlusion.
Pegaptanib (Macugen®) was FDA approved for the treatment of neovascular (wet) age-related macular degeneration (AMD) in December 2004.
Indications
- diabetic macular edema
- diabetic retinopathy
- macular degeneration
NOTE: Prior to intravitreal injection, prepare the eye with a local anesthetic and povidone iodine and/or a broad spectrum antibiotic (see Administration).
NOTE: Following the injection, monitor patient for elevation in intraocular pressure (IOP) and endophthalmitis (see Adverse Reactions).
For the treatment of neovascular (wet) age-related macular degeneration (AMD)
Side Effects
- anaphylactic shock
- anaphylactoid reactions
- angioedema
- blepharitis
- blurred vision
- cataracts
- chest pain (unspecified)
- conjunctivitis
- contact dermatitis
- corneal deposits
- corneal edema
- diabetes mellitus
- diarrhea
- dizziness
- dyspepsia
- endophthalmitis
- headache
- hearing loss
- hypertension
- infection
- keratitis
- mydriasis
- myocardial infarction
- nausea
- ocular discharge
- ocular hemorrhage
- ocular hypertension
- ocular infection
- ocular inflammation
- ocular irritation
- ocular pain
- photopsia
- pleural effusion
- retinal detachment
- retinal edema
- stroke
- urinary retention
- vertigo
- visual impairment
- vomiting
Monitoring Parameters
- intraocular pressure
Contraindications
- breast-feeding
- cataracts
- children
- glaucoma
- increased intraocular pressure
- ocular infection
- ocular surgery
- pregnancy
Pegaptanib is contraindicated in patients with hypersensitivity to pegaptanib or any of the components of the product.
Interactions
There are no drug interactions associated with Pegaptanib products.
