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Namespace Prefixes

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Statements

Subject Item
n2:DB04895
rdf:type
n3:Drug
n3:description
Pegaptanib is a polynucleotide aptamer. Pegaptanib 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]
n3:dosage
n16:271B5DE3-363D-11E5-9242-09173F13E4C5 n16:271B5DE4-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Vinores SA: Pegaptanib in the treatment of wet, age-related macular degeneration. Int J Nanomedicine. 2006;1(3):263-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17717967 # Wylegala E, Teper SJ: [VEGF in age-related macular degeneration. Part II. VEGF inhibitors use in age-related macular degeneration treatment] Klin Oczna. 2007;109(1-3):97-100. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17687925 # Bakri SJ, Pulido JS, McCannel CA, Hodge DO, Diehl N, Hillemeier J: Immediate intraocular pressure changes following intravitreal injections of triamcinolone, pegaptanib, and bevacizumab. Eye. 2007 Aug 10;. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17693999 #Dynamed #Product monograph #Lexicomp
n3:group
investigational approved
n3:halfLife
In humans, after a 3 mg monocular dose (10 times the recommended dose), the average (± standard deviation) apparent plasma half-life of pegaptanib is 10 (± 4) days.
n3:indication
For the treatment of neovascular (wet) age-related macular degeneration.
owl:sameAs
n12:DB04895 n17:DB04895
dcterms:title
Pegaptanib
adms:identifier
n5:PA164771236 n20:DB04895 n21:Pegaptanib
n3:mechanismOfAction
Pegaptanib sodium is a pegylated aptamer, a modified oligonucleotide, which adopts a three- dimensional conformation that enables it to bind to extracellular VEGF with high affinity and selectivity. Pegaptanib sodium binds to the major pathological VEGF isoform, extracellular VEGF165, with high affinity (Kd = 200 pM) and specificity, thereby inhibiting VEGF165 binding to its VEGF receptors. In contrast virtually no binding of the non-pegylated aptamer to VEGF121 or the VEGF -related proteins VEGF-B, VEGF-C and placental growth factor (PlGF) was detected using invitro filter binding assays. Pegaptanib sodium does not bind significantly to VEGF121. In animal models, VEGF164 (the rodent counterpart of human VEGF165) was specifically upregulated in disease. The selective inhibition of VEGF164 with pegaptanib sodium proved as effective at suppressing pathological neovascularization as pan-VEGF inhibition7, however pegaptanib sodium spared the normal vasculature whereas pan-VEGF inhibition did not.
n3:packager
n9:271B5DE1-363D-11E5-9242-09173F13E4C5 n9:271B5DDF-363D-11E5-9242-09173F13E4C5 n9:271B5DE0-363D-11E5-9242-09173F13E4C5
n3:patent
n10:2269072 n10:6011020 n10:6147204
n3:routeOfElimination
It is excreted primarily in urine as unchanged drug and also as metabolites. There is no dosage adjustment required for patients with renal impairment although it must be noted that not many studies have looked at patients with a creatinine clearance of 30mL/min.
n3:synonym
Pegaptanib sodium NX1838 EYE 001 NX 1838 Pegaptanib Octasodium
n3:toxicity
It is not known if pegaptanib is safe in pregnant women or if it is excreted in breast milk. Likewise, no studies have been done in the pediatric population. Most adverse events elated to the drug are ocular however non-ocular adverse events related to the drug or the injection procedure also occurred, among which headaches and rhinorrhoea appeared in more than 1% of patients. Pegaptanib is contraindicated when the patient has an ocular or periocular infection.
n3:volumeOfDistribution
It is distributed into vitreous fluid, retina, aqueous fluid, and kidneys. As well, it has been shown to cross the placenta in mice but whether or not it crosses the placenta in humans is unknown.
foaf:page
n14:macugen.htm n19:pegaptanib.html
n3:Molecular-Formula
n15:271B5DE6-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n15:271B5DE5-363D-11E5-9242-09173F13E4C5
n7:hasATCCode
n8:S01LA03
n3:absorption
In animals, pegaptanib is slowly absorbed into the systemic circulation from the eye after intravitreous administration.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
222716-86-1
n3:containedIn
n6:271B5DE2-363D-11E5-9242-09173F13E4C5