About: Pegaptanib     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/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] (en)
http://linked.open...y/drugbank/dosage
http://linked.open...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 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/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. (en)
http://linked.open...ugbank/indication
  • For the treatment of neovascular (wet) age-related macular degeneration. (en)
sameAs
Title
  • Pegaptanib (en)
adms:identifier
http://linked.open...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. (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • 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. (en)
http://linked.open.../drugbank/synonym
  • EYE 001 (en)
  • NX 1838 (en)
  • NX1838 (en)
  • Pegaptanib Octasodium (en)
  • Pegaptanib sodium (en)
http://linked.open...drugbank/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. (en)
http://linked.open...umeOfDistribution
  • 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. (en)
foaf:page
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...l/drug/hasATCCode
http://linked.open...ugbank/absorption
  • In animals, pegaptanib is slowly absorbed into the systemic circulation from the eye after intravitreous administration. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 222716-86-1 (en)
http://linked.open...gbank/containedIn
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