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Macugen: Full Drug Profile

Medically reviewed by Min Clinic Staff | Updated: January 2026

Macugen - General Information

Macugen is a pegylated anti-VEGF aptamer, a single strand of nucleic acid that binds with specificity to a particular target. Macugen specifically binds to VEGF 165, a protein that plays a critical role in angiogenesis (the formation of new blood vessels) and increased permeability (leakage from blood vessels), two of the primary pathological processes responsible for the vision loss associated with neovascular AMD. [Wikipedia]

 

Pharmacology of Macugen

Macugen is a selective vascular endothelial growth factor (VEGF) antagonist. VEGF is a secreted protein that selectively binds and activates its receptors located primarily on the surface of vascular endothelial cells. VEGF induces angiogenesis, and increases vascular permeability and inflammation, all of which are thought to contribute to the progression of the neovascular (wet) form of age-related macular degeneration (AMD), a leading cause of blindness. VEGF has been implicated in blood retinal barrier breakdown and pathological ocular neovascularization.

 

Additional information about Macugen

Macugen Indication: For the treatment of neovascular (wet) age-related macular degeneration. Mechanism Of Action: Macugen binds to the major pathological VEGF isoform, extracellular VEGF165, thereby inhibiting VEGF165 binding to its VEGF receptors. The inhibition of VEGF164, the rodent counterpart of human VEGF165, was effective at suppressing pathological neovascularization. Drug Interactions: Not Available Food Interactions: Not Available Generic Name: Pegaptanib Synonyms: Not Available Drug Category: Not Available Drug Type: Biotech; Approved; Investigational Other Brand Names containing Pegaptanib: Macugen; Absorption: In animals, pegaptanib is slowly absorbed into the systemic circulation from the eye after intravitreous administration. Toxicity (Overdose): Not Available Protein Binding: Not Available Biotransformation: Based on preclinical data, pegaptanib is metabolized by endo- and exonucleases. Half Life: In humans, after a 3 mg monocular dose (10 times the recommended dose), the average (& Dosage Forms of Macugen: Solution Intravitreal Chemical IUPAC Name: Not Available Chemical Formula: Not Available Pegaptanib on Wikipedia: https://en.wikipedia.org/wiki/Pegaptanib Organisms Affected: Humans and other mammals