Pegaptanib Sodium

Synonyms: EYE-001; Natrii Pegaptanibum; NX-1838; Pegaptanib Octasodium; Pegaptanib sodico; Pégaptanib Sodique.
Cyrillic synonym: Натрий Пегаптаниб.

💊 Chemical information

CAS — 222716-86-1.
ATC — S01LA03.
ATC Vet — QS0 1LA03.

💊 Adverse Effects and Precautions

Endophthalmitis has been reported in patients given pegaptanib sodium and patients should be monitored for signs of infections for a week after the procedure. Retinal haemorrhage, retinal detachment, iatrogenic traumatic cataract, and raised intra-ocular pressure have also been reported. Immediate or delayed intravitreous haemorrhage may occur after injection. Common but less serious ocular adverse effects include eye pain, irritation, inflammation, blurred vision, visual disturbances, corneal oedema, punctate keratitis, and vitreous floaters. Non-ocular adverse effects that have been reported include headache, rhinorrhoea, bronchitis, diarrhoea, dizziness, nausea, and urinary-tract infections. Hypersensitivity reactions, including anaphylaxis or anaphylactoid reactions, and angioedema have been reported rarely within several hours of a dose. Pegaptanib is contra-indicated in patients with active or suspected ocular or periocular infections. The most common ocular adverse effects were attributed to the injection procedure and were transient and mild to moderate in intensity. Failure to follow the injection preparation protocol accounted for most cases of endophthalmitis. The incidence of adverse effects associated with systemic inhibition of vascular endothelial growth factor or severe ocular inflammation, cataract progression, or glaucoma was not higher in the pegaptanib-treated patients compared with patients receiving sham injections. Overall, the safety profile of pegaptanib was favourable in these studies.
1. D’Amico DJ, et al. VEGF Inhibition Study in Ocular Neovascularization (V.I.S.I.O.N.) Clinical Trial Group. Pegaptanib sodium for neovascular age-related macular degeneration: two-year safety results of the two prospective, multicenter, controlled clinical trials. Ophthalmology 2006; 113: 992–1001.

💊 Uses and Administration

Pegaptanib is a pegylated modified oligonucleotide (aptamer) given as the sodium salt in the treatment of neovascular (wet) age-related macular degeneration. It is given by intravitreal injection into the affected eye in a dose of 300 micrograms once every 6 weeks. Stopping or withholding treatment should be considered if there has been no demonstrable benefit after 2 consecutive injections (i.e. at the 12-week visit). Pegaptanib is also under investigation as an adjunct in the management of diabetic retinopathy.

Age-related macular degeneration.

Pegaptanib is a pegylated modified oligonucleotide (aptamer) used in the treatment of age-related macular degeneration (AMD). It binds to and inhibits vascular endothelial growth factor (VEGF), which is a stimulant of angiogenesis thought to play a role in the neovascularisation and retinal changes associated with AMD. Pegaptanib is a selective antagonist of VEGF.1,2 Positive outcomes have been reported from two concurrent international multicentre prospective randomised controlled studies.3Vision loss was prevented and mean visual acuity improved in patients given 6-weekly injections of 300 micrograms, 1 mg, or 3 mg for 48 weeks compared with patients receiving sham injections. No dose-response relationship was found. In order to assess the effects of long-term therapy, patients who had been given pegaptanib in the first part of the study were then randomised at week 54 to receive either pegaptanib for a further 48 weeks or stop treatment, and patients who had been given sham injections were similarly re-randomised.4 Results showed that patients given pegaptanib for a second year continued to derive additional benefit. A systematic review5 of 5 randomised controlled studies found that pegaptanib was effective in reducing the risk of loss of visual acuity.
1. Siddiqui MAA, Keating GM. Pegaptanib: in exudative age-related macular degeneration. Drugs 2005; 65: 1571–7
2. Chapman JA, Beckey C. Pegaptanib: a novel approach to ocular neovascularization. Ann Pharmacother 2006; 40: 1322–6
3. Gragoudas ES, et al. Pegaptanib for neovascular age-related macular degeneration. N Engl J Med 2004; 351: 2805–16
4. Chakravarthy U, et al.. VEGF Inhibition Study in Ocular Neovascularization (V.I.S.I.O.N.) Clinical Trial Group. Year 2 efficacy results of 2 randomized controlled clinical trials of pegaptanib for neovascular age-related macular degeneration. Ophthalmology 2006; 113: 1508–21
5. Vedula SS, Krzystolik MG. Antiangiogenic therapy with antivascular endothelial growth factor modalities for neovascular age-related macular degeneration. Available in The Cochrane Database of Systematic Reviews; Issu
2. Chichester: John Wiley; 2008 (accessed 06/06/08).

💊 Preparations

Proprietary Preparations

Braz.: Macugen; Canad.: Macugen; Cz.: Macugen; Fr.: Macugen; Gr.: Macugen; Pol.: Macugen; Port.: Macugen; Singapore: Macugen; UK: Macugen; USA: Macugen.
Published May 08, 2019.