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Anti-VEGF (RNA Aptamer) — Neovascular AMD Pregnancy: No data — AMD is a disease of older adults; not typically applicable; anti-VEGF agents theoretically teratogenic

Pegaptanib Sodium

Brand names: Macugen

Adult dose

Dose: 0.3 mg intravitreal injection every 6 weeks
Route: Intravitreal injection (administered by specialist)
Frequency: Every 6 weeks
Max: 0.3 mg per injection
First anti-VEGF agent approved for neovascular AMD (FDA 2004, EMA 2006); selectively inhibits VEGF165 isoform only; largely superseded by ranibizumab and aflibercept for superior efficacy; remains in BNF 90; historical significance as founding agent of anti-VEGF class

Paediatric dose

Route: N/A
Frequency: N/A
Max: Not indicated in children
AMD is a disease of older adults; no paediatric indication

Dose adjustments

Renal

No dose adjustment (local delivery, minimal systemic exposure)

Hepatic

No dose adjustment

Clinical pearls

  • Pharmacological landmark: pegaptanib was the FIRST anti-VEGF treatment approved for any indication — FDA approval December 2004 (neovascular AMD); it validated the VEGF pathway as a therapeutic target in eye disease and established intravitreal injection as a viable clinical delivery route for large molecules
  • RNA aptamer mechanism: pegaptanib is a polyethylene glycol-conjugated synthetic RNA oligonucleotide (aptamer) that selectively binds and neutralises VEGF165 isoform — differs fundamentally from ranibizumab (antibody fragment) and aflibercept (fusion protein) which block multiple VEGF isoforms
  • VISION trials (NEJM 2004): showed 70% of patients maintained vision vs ~55% sham; statistically significant benefit; however, only ~6% improved vision (vs 34% with ranibizumab in MARINA/ANCHOR) — the agent stabilises rather than substantially improves vision
  • Superseded but not withdrawn: ranibizumab (Lucentis) and aflibercept (Eylea) substantially outperform pegaptanib — pegaptanib is rarely used in modern practice; knowledge of pegaptanib remains clinically relevant for understanding anti-VEGF class pharmacology, historical context, and patients who may have received it during the mid-2000s
  • VEGF165 selectivity: pegaptanib binds only VEGF165 (most pro-angiogenic isoform) — leaves VEGF121 and VEGF189 isoforms intact; VEGF isoforms have physiological roles in neuroprotection and vascular maintenance; selective inhibition was theoretically more targeted, but in practice less efficacious than pan-VEGF blockade

Contraindications

  • Ocular or periocular infection
  • Active severe intraocular inflammation
  • Hypersensitivity to pegaptanib or any excipient

Side effects

  • Endophthalmitis (intravitreal injection risk)
  • Traumatic cataract
  • Increased IOP
  • Conjunctival haemorrhage
  • Eye pain
  • Reduced visual acuity (treatment failure)

Interactions

  • No significant drug interactions — local intravitreal delivery

Monitoring

  • Visual acuity at each visit (ETDRS chart)
  • OCT for macular fluid
  • IOP post-injection
  • Signs of endophthalmitis (pain, redness, photophobia)

Reference: BNFc; BNF 90; FDA Approval Macugen December 2004; EMA Approval 2006; Gragoudas et al. NEJM 2004 (VISION trial); SPC Macugen. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.

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