Pegaptanib

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Macugen; Belgium: Macugen; Czech Republic: Macugen; Denmark: Macugen; Estonia: Macugen; Finland: Macugen; France: Macugen; Germany: Macugen; Greece: Macugen; Hungary: Macugen; Ireland: Macugen; Italy: Macugen; Latvia: Macugen; Lithuania: Macugen; Luxembourg: Macugen; Malta: Macugen; Netherlands: Macugen; Poland: Macugen; Portugal: Macugen; Romania: Macugen; Slovakia: Macugen; Slovenia: Macugen; Spain: Macugen; Sweden: Macugen; UK: Macugen.

North America

Canada: Macugen; USA: Macugen.

Latin America

Brazil: Macugen.

Asia

Japan: Macugen.

Drug combinations

Chemistry

Pegaptanib Sodium: C~294~H~342~F~13~N~107~Na~28~O~188~P~28~ [C~2~H~4~O]~n~. Mw: approx. 50,000.01. (1) RNA, ((2′-Deoxy-2′-fluoro)C-G~m~-G~m~-A-A-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)C-A~m~-G~m~-(2′-deoxy-2′-fluoro)U-G~m~-A~m~-A~m~-(2′-deoxy-2’2′-fluoro)U-G~m~-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)U-A~m~-(2′-deoxy-2′-fluoro)U-A~m~-(2′-deoxy-2′-fluoro)C-A~m~-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)C-G~m~-(3→3′)-dT), 5′-ester with α,α»-[4,12-dioxo-6-[[[5-(phosphoonoxy)pentyl]amino]carbonyl]-3,13-dioxa-5,11-diaza-1,15-pentadecanediyl]bis[ω-methoxypoly(oxy-1,2-ethanediyl)], sodium salt; (2) 5′-Ester of (2′-deoxy-2′-fluoro)C-G~m~-G~m~-A-A-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)C-A~m~-G~m~-(2′-deoxy-2′-fluoro)U-G~m~-A~m~-A~m~-(2′-deoxy-2′-fluoro)U-G~m~-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)U-A~m~-(2′-deoxy-2′-fluoro)U-A~m~-(2′-deoxy-2′-fluoro)C-A~m~-(2′-deoxy-2′-fluoro)U-(2’2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)C-G~m~-(3’→3′)-dT with α,α’-[[(1S)-1-[[5-(phosphonooxy)pentyl]carbamoyl]pentane-1,5-diyl]bis(iminocarbonyl)]bis[ω-methoxypoly(oxyethane-1,2-diyl)] sodium salt. CAS-222716-86-1 (2002).

Pharmacologic Category

EENT Drugs, Miscellaneous. Ophthalmic Agent; Vascular Endothelial Growth Factor Inhibitor. (ATC-Code: S01LA03).

Mechanism of action

Pegaptanib binds to extracellular endothelial growth factor, inhibiting vascular endothelial growth factor from binding to its receptors and thereby suppressing neovascularization and slowing vision loss.

Therapeutic use

Treatment of neovascular (wet) age-related macular degeneration.

Pregnancy and lactiation implications

Teratogenic effects not reported in animal studies. There are no adequate, well-controlled studies in pregnant women. Excretion in breast milk unknown (use caution).

Unlabeled use

Contraindications

Hypersensitivity to pegaptanib or any component of the formulation. Ocular or periocular infection.

Warnings and precautions

Intravitreous injections may be associated with endophthalmitis. Rare hypersensitivity reactions (including anaphylaxis) associated with use. Following injection, intraocular pressure may increase.

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