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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.


  • 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

  1. anaphylactic shock
  2. anaphylactoid reactions
  3. angioedema
  4. blepharitis
  5. blurred vision
  6. cataracts
  7. chest pain (unspecified)
  8. conjunctivitis
  9. contact dermatitis
  10. corneal deposits
  11. corneal edema
  12. diabetes mellitus
  13. diarrhea
  14. dizziness
  15. dyspepsia
  16. endophthalmitis
  17. headache
  18. hearing loss
  19. hypertension
  20. infection
  21. keratitis
  22. mydriasis
  23. myocardial infarction
  24. nausea
  25. ocular discharge
  26. ocular hemorrhage
  27. ocular hypertension
  28. ocular infection
  29. ocular inflammation
  30. ocular irritation
  31. ocular pain
  32. photopsia
  33. pleural effusion
  34. retinal detachment
  35. retinal edema
  36. stroke
  37. urinary retention
  38. vertigo
  39. visual impairment
  40. vomiting

Monitoring Parameters

  • intraocular pressure


  • 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.


There are no drug interactions associated with Pegaptanib products.

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