Pharmacokinetic evaluation of pegaptanib octasodium for the treatment of diabetic edema

Expert Opin Drug Metab Toxicol. 2014 Aug;10(8):1185-92. doi: 10.1517/17425255.2014.922543. Epub 2014 May 24.

Abstract

Introduction: Diabetic macular edema (DME) is a leading cause of visual impairment in patients with diabetic retinopathy. Pegaptanib octasodium (Macugen) was the first anti-VEGF agent approved for the treatment of neovascular age-related macular degeneration. It is a selective anti-VEGF agent, which only blocks VEGF. It has been shown to be safe and effective in treatment of DME in randomized controlled trials and it may be a safer first-line treatment in patients with diabetes with a predisposition to cardiovascular risk factors.

Areas covered: This review covers the pharmacokinetics of pegaptanib octasodium. The authors also evaluate pegaptanib octasodium's clinical efficacy, safety and tolerability in DME.

Expert opinion: DME is the most common cause of visual loss in patients with diabetes. Pegaptanib has been found to be more effective than laser therapy alone for center-involving DME, its efficacy might be slightly worse than other pan-VEGF blockers, but the number of patients that have significant improvement of vision after treatment are similar to those treated with pan-VEGF blockers. As a selective VEGF blocker, it may have a better ocular and systemic safety profile than pan-VEGF blocking agents. It is reasonable to consider pegaptanib as the first-line treatment for center-involving DME with pan-VEGF blockers reserved for non-responders.

Keywords: Macugen; diabetic macular edema; expert review; pegaptanib octasodium.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Aptamers, Nucleotide / adverse effects
  • Aptamers, Nucleotide / pharmacokinetics*
  • Aptamers, Nucleotide / therapeutic use
  • Cardiovascular Diseases / etiology
  • Diabetic Retinopathy / drug therapy*
  • Diabetic Retinopathy / pathology
  • Humans
  • Macular Degeneration / drug therapy
  • Macular Degeneration / pathology
  • Macular Edema / drug therapy*
  • Macular Edema / etiology
  • Macular Edema / pathology
  • Risk Factors
  • Vascular Endothelial Growth Factor A / antagonists & inhibitors
  • Vision Disorders / drug therapy
  • Vision Disorders / etiology

Substances

  • Aptamers, Nucleotide
  • Vascular Endothelial Growth Factor A
  • pegaptanib