2000
DOI: 10.1023/a:1007657109012
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Abstract: The no observable effect level was greater than six biweekly bilateral 0.50 mg/eye doses or two biweekly bilateral 1.0 mg/eye doses. These pharmacokinetic and safety data support monthly 1 or 2 mg/eye dose regimens in human clinical trials.

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Cited by 171 publications
(48 citation statements)
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“…Four anti-VEGF pharmacologic agents are now commercially available and being in use in trials for treatment of diabetic macular edema (DME) and PDR. Pegaptanib ( Macugen , OSI/Eyetech, Melville, NY, USA) is a modified 28-base RNA aptamer, which binds to VEGF 165 isoform inhibiting its vascular permeability effects [180]. Pegaptanib was tested in vitro which showed significance inhibition of VEGF induced vascular permeability [181].…”
Section: Treatment Of Retinal Neovascularizationmentioning
confidence: 99%
“…Four anti-VEGF pharmacologic agents are now commercially available and being in use in trials for treatment of diabetic macular edema (DME) and PDR. Pegaptanib ( Macugen , OSI/Eyetech, Melville, NY, USA) is a modified 28-base RNA aptamer, which binds to VEGF 165 isoform inhibiting its vascular permeability effects [180]. Pegaptanib was tested in vitro which showed significance inhibition of VEGF induced vascular permeability [181].…”
Section: Treatment Of Retinal Neovascularizationmentioning
confidence: 99%
“…The observation that the VEGF aptamer remains active and can be recovered from the vitreous humour of rhesus monkeys 28 days after injection [53] is encouraging with regard to prospects for long-term ocular retention of the compound. Because most existing drugs are protein antagonists, the ultimate success of aptamers as therapeutic agents will probably depend on how well they compete with other classes of therapeutic compounds.…”
Section: Pegaptanib (Macugen): Breakthrough In the Therapeutic Applicmentioning
confidence: 98%
“…The advantages include high specificity and binding affinity for the target antigen, minimal immunogenicity, and easy modification (Drolet et al, 2000; Torchilin, 2005). Aptamers are stable over wide temperature and pH ranges, and they are stable in organic solvents (Nimjee et al, 2005; Wilson and Szostak, 1998).…”
Section: Targeting Moietiesmentioning
confidence: 99%