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Description

pegaptanib: a 28-base ribonucleic acid aptamer covalently linked to two branched 20-kD polyethylene glycol moieties to block the activity of extracellular VEGF, specifically the 165-amino-acid isoform (VEGF165); for treatment of neovascular age-related macular degeneration [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID56603655
MeSH IDM0128441

Synonyms (8)

Synonym
pegaptanib sodium
pegaptanib
macugen
eyeoo1
nx183
7-[[(2s)-2,6-bis(2-methoxyethoxycarbonylamino)hexanoyl]amino]heptoxy-methylphosphinic acid
gtpl6836
Q27088289

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"All reported adverse events, serious adverse events, and deaths."( Pegaptanib sodium for neovascular age-related macular degeneration: two-year safety results of the two prospective, multicenter, controlled clinical trials.
Adamis, AP; Cunningham, ET; D'Amico, DJ; Guyer, DR; Katz, B; Masonson, HN; Patel, M, 2006
)
0.33
" The most common ocular adverse events were transient, mild to moderate in intensity, and attributed to the injection preparation and procedure."( Pegaptanib sodium for neovascular age-related macular degeneration: two-year safety results of the two prospective, multicenter, controlled clinical trials.
Adamis, AP; Cunningham, ET; D'Amico, DJ; Guyer, DR; Katz, B; Masonson, HN; Patel, M, 2006
)
0.33
" Visual acuity measurements, biomicroscopy, funduscopy, fluorescein angiography, optical coherence tomography, and adverse event assessments were performed."( Safety and efficacy of intravitreal bevacizumab followed by pegaptanib maintenance as a treatment regimen for age-related macular degeneration.
Hughes, MS; Sang, DN,
)
0.13
" Adverse events were limited to transient irritation or redness."( Safety and efficacy of intravitreal bevacizumab followed by pegaptanib maintenance as a treatment regimen for age-related macular degeneration.
Hughes, MS; Sang, DN,
)
0.13
"Safety assessments included blood chemistries, urinalyses, vital signs, electrocardiograms, serum antipegaptanib antibody assays, adverse events, VAs, and intraocular pressures."( Pegaptanib 1-year systemic safety results from a safety-pharmacokinetic trial in patients with neovascular age-related macular degeneration.
Adamis, AP; Apte, RS; Masonson, H; Modi, M; Patel, M; Whitfield, L, 2007
)
0.34
" Few systemic adverse events were noted."( Pegaptanib 1-year systemic safety results from a safety-pharmacokinetic trial in patients with neovascular age-related macular degeneration.
Adamis, AP; Apte, RS; Masonson, H; Modi, M; Patel, M; Whitfield, L, 2007
)
0.34
" Most ocular adverse events were related to the injection procedure itself and were mild or moderate in severity."( Pegaptanib 1-year systemic safety results from a safety-pharmacokinetic trial in patients with neovascular age-related macular degeneration.
Adamis, AP; Apte, RS; Masonson, H; Modi, M; Patel, M; Whitfield, L, 2007
)
0.34
"These studies, together with data from clinical trials, provide strong evidence that inhibition of VEGF(165) by pegaptanib in the eye is a safe therapy for the treatment of ocular neovascular disease."( Local tolerance and systemic safety of pegaptanib sodium in the dog and rabbit.
Foy, JW; Modi, M; Patel, M; Rittenhouse, K, 2007
)
0.34
" Adverse events were mainly ocular in nature, mild, transient and injection-related."( Pegaptanib sodium for neovascular age-related macular degeneration: third-year safety results of the VEGF Inhibition Study in Ocular Neovascularisation (VISION) trial.
Adamis, AP; Buggage, R; Cunningham, E; Goldbaum, M; Guyer, D; Katz, B; Masonson, H; Patel, M; Singerman, LJ, 2008
)
0.35
"Review of current literature suggests that intravitreal antivascular endothelial growth factor agents are generally a safe and effective treatment for neovascular AMD for up to 2-3 years."( Safety and efficacy of intravitreal anti-VEGF injections for age-related macular degeneration.
Jeganathan, VS; Verma, N, 2009
)
0.35
"The off-label use of Avastin eye drops and GS101 eye drops against insulin receptor substrate (IRS)-1, which have been tested in phase II trial, both seem to be relatively efficient and safe ways to inhibit progressive corneal neovascularisation."( [Topical inhibition of angiogenesis at the cornea. Safety and efficacy].
Bachmann, B; Bock, F; Cursiefen, C; Hos, D; König, Y; Parthasarathy, A; Regenfuss, B, 2009
)
0.35
" However, within these trials, there is some circumstantial evidence that links systemic VEGF inhibition to systemic adverse events, particularly systemic thromboembolic events."( Safety implications of vascular endothelial growth factor blockade for subjects receiving intravitreal anti-vascular endothelial growth factor therapies.
Csaky, K; Do, DV, 2009
)
0.35
"Even at higher doses, bevacizumab and ranibizumab showed no toxic effects on RGC in vivo in either untreated rats or in the NMDA-induced RGC damage model."( Toxicity testing of the VEGF inhibitors bevacizumab, ranibizumab and pegaptanib in rats both with and without prior retinal ganglion cell damage.
Bartz-Schmidt, KU; Bolz, S; Choragiewicz, TJ; Fiedorowicz, M; Henke-Fahle, S; Schuettauf, F; Thaler, S; Tura, A; Yoeruek, E; Ziemssen, F; Zrenner, E, 2010
)
0.36
" For ranibizumab, the principal ocular adverse event detected in clinical trials was a low frequency of ocular inflammation, and systemic adverse events included a slightly elevated risk of nonocular hemorrhage and stroke."( Systemic and ocular safety of intravitreal anti-VEGF therapies for ocular neovascular disease.
Tolentino, M,
)
0.13
" The number of responders and adverse events were monitored."( [Long-term efficacy and safety profile of pegaptanib sodium for age-related macular degeneration with choroidal neovascularization--evaluation of extended phase II clinical trial].
, 2011
)
0.37
" The objective of the present study was to systematically assess and compare the incidences of adverse events of anti-VEGFs."( A systematic review of the adverse events of intravitreal anti-vascular endothelial growth factor injections.
De Jong-Hesse, Y; Hendrikse, F; La Heij, EC; Ringens, PJ; Schouten, JS; van der Reis, MI, 2011
)
0.37
" We used the terms pegaptanib, bevacizumab, ranibizumab, intravitreal, and specific and general terms for adverse events."( A systematic review of the adverse events of intravitreal anti-vascular endothelial growth factor injections.
De Jong-Hesse, Y; Hendrikse, F; La Heij, EC; Ringens, PJ; Schouten, JS; van der Reis, MI, 2011
)
0.37
"Two hundred and seventy-eight articles were included, and the incidences of adverse events were calculated separately for effect, safety, and specific side effect studies."( A systematic review of the adverse events of intravitreal anti-vascular endothelial growth factor injections.
De Jong-Hesse, Y; Hendrikse, F; La Heij, EC; Ringens, PJ; Schouten, JS; van der Reis, MI, 2011
)
0.37
"The reported rates of serious adverse events were low after anti-VEGF injections."( A systematic review of the adverse events of intravitreal anti-vascular endothelial growth factor injections.
De Jong-Hesse, Y; Hendrikse, F; La Heij, EC; Ringens, PJ; Schouten, JS; van der Reis, MI, 2011
)
0.37
" Adverse events were summarized from the first injection to 42 days after the last injection."( A retrospective, pooled data analysis of the safety of pegaptanib sodium in the treatment of age-related macular degeneration in subjects with or without diabetes mellitus.
Dombi, T; Kwok, KK; Sultan, MB, 2012
)
0.38
"Pegaptanib proved to be efficacious and safe for the treatment of diabetic macular edema throughout the 12-month followup."( Efficacy and safety of the intravitreal treatment of diabetic macular edema with pegaptanib: a 12-month follow-up.
Brillante, C; De Paolis, G; Impallara, D; La Torre, G; Malarska, K; Muscella, R; Pacella, E; Pacella, F; Smaldone, G; Turchetti, P, 2013
)
0.39
" Pre-marketing, phase III randomized controlled trials (RCT), postmarketing clinical trials, observational longitudinal studies, and case reports involving adverse events (AE) were included."( Safety monitoring of ophthalmic biologics: a systematic review of pre- and postmarketing safety data.
Alves, C; Batel Marques, F; Mendes, D; Penedones, A, 2014
)
0.4
"The purpose of this study is to conduct a comparative analysis of the suspected adverse drug reactions (ADRs) associated with intravitreal bevacizumab, ranibizumab and pegaptanib in the WHO database in order to have a real-life information on these drugs, which now is only based on data coming from clinical trials."( Comparative safety profiles of intravitreal bevacizumab, ranibizumab and pegaptanib: the analysis of the WHO database of adverse drug reactions.
Amato, R; Biagi, C; Buccellato, E; Conti, V; Covezzoli, A; Donati, M; Melis, M; Montanaro, N; Motola, D; Pazzi, L; Vaccheri, A; Venegoni, M, 2014
)
0.4
" Treatment safety was estimated using the proportions of adverse events, namely increased intraocular pressure (IOP), cataracts, vitreous haemorrhage (VH) and retinal tear."( Comparison of the efficacy and safety of drug therapies for macular edema secondary to central retinal vein occlusion.
Li, M; Qian, T; Wan, Y; Xu, X; Zhao, M, 2018
)
0.48

Pharmacokinetics

ExcerptReferenceRelevance
" The mean apparent terminal half-life was 10 days."( Pegaptanib 1-year systemic safety results from a safety-pharmacokinetic trial in patients with neovascular age-related macular degeneration.
Adamis, AP; Apte, RS; Masonson, H; Modi, M; Patel, M; Whitfield, L, 2007
)
0.34
" Therefore, a population pharmacokinetic (PK) analysis of pegaptanib was undertaken in Western and Asian AMD patients to determine the influence of renal function on apparent pegaptanib clearance (CL)."( Population pharmacokinetics of pegaptanib in patients with neovascular, age-related macular degeneration.
Basile, AS; Hutmacher, M; Kowalski, K; Masayo, O; Nakane, M; Nickens, D; Nielsen, J; Whitfield, L, 2012
)
0.38
"To use novel OCT parameters in assessing the differential pharmacodynamic effects of bevacizumab (Avastin; Genentech, South San Francisco, CA), pegaptanib (Macugen; OSI Pharmaceuticals, New York, NY), and verteporfin photodynamic therapy (PDT; Novartis, Basel, Switzerland) in a recently completed phase III/IV clinical trial."( Assessment of differential pharmacodynamic effects using optical coherence tomography in neovascular age-related macular degeneration.
Heussen, FM; Keane, PA; Mokwa, N; Ouyang, Y; Patel, PJ; Sadda, SR; Tufail, A; Walsh, AC, 2012
)
0.38
" In the emerging era of neovascular AMD therapeutics, the capacity of OCT to provide such detailed pharmacodynamic information in a noninvasive manner is likely to attain increased importance."( Assessment of differential pharmacodynamic effects using optical coherence tomography in neovascular age-related macular degeneration.
Heussen, FM; Keane, PA; Mokwa, N; Ouyang, Y; Patel, PJ; Sadda, SR; Tufail, A; Walsh, AC, 2012
)
0.38

Compound-Compound Interactions

ExcerptReferenceRelevance
"To evaluate the effectiveness of pegaptanib combined with intravitreal injection of moxifloxacin as treatment of wet macular degeneration."( Pegaptanib combined with intravitreal injection of moxifloxacin as treatment of wet macular degeneration.
Bennett, MD; Bryan, JS; Yee, W,
)
0.13
"This retrospective review included patients who received pegaptanib combined with 165 microg of moxifloxacin every 6 weeks."( Pegaptanib combined with intravitreal injection of moxifloxacin as treatment of wet macular degeneration.
Bennett, MD; Bryan, JS; Yee, W,
)
0.13
"Pegaptanib combined with intravitreal injection of moxifloxacin appears to be effective treatment of wet macular degeneration."( Pegaptanib combined with intravitreal injection of moxifloxacin as treatment of wet macular degeneration.
Bennett, MD; Bryan, JS; Yee, W,
)
0.13
"To investigate efficacy of intravitreal injection of pegaptanib and laser photocoagulation for treatment of stage 3+ retinopathy of prematurity (ROP) affecting zone I and posterior zone II, and to compare the results in terms of regression, development of peripheral retinal vessels, and final structural outcome with conventional laser photocoagulation or combined with cryotherapy."( Intravitreal pegaptanib combined with diode laser therapy for stage 3+ retinopathy of prematurity in zone I and posterior zone II.
Autrata, R; Borek, I; Doležel, Z; Holoušová, M; Krejcírová, I; Senková, K,
)
0.13
"02 mL, Pfizer) with conventional diode laser photocoagulation in group 1 (68 eyes of 34 infants) or only laser therapy combined with cryotherapy in group 2 (84 eyes of 42 infants), bilaterally."( Intravitreal pegaptanib combined with diode laser therapy for stage 3+ retinopathy of prematurity in zone I and posterior zone II.
Autrata, R; Borek, I; Doležel, Z; Holoušová, M; Krejcírová, I; Senková, K,
)
0.13

Bioavailability

ExcerptReferenceRelevance
" Their affinity and specificity for a given protein make it possible to isolate a ligand to virtually any target, and adjusting their bioavailability expands their clinical utility."( Aptamers: an emerging class of therapeutics.
Nimjee, SM; Rusconi, CP; Sullenger, BA, 2005
)
0.33
" A 1-compartment model parameterized in terms of the absorption rate constant, apparent volume of distribution, and CL was used to describe the pegaptanib plasma concentration data."( Population pharmacokinetics of pegaptanib in patients with neovascular, age-related macular degeneration.
Basile, AS; Hutmacher, M; Kowalski, K; Masayo, O; Nakane, M; Nickens, D; Nielsen, J; Whitfield, L, 2012
)
0.38

Dosage Studied

ExcerptRelevanceReference
"In the combined analysis of the primary end point (for a total of 1186 patients), efficacy was demonstrated, without a dose-response relationship, for all three doses of pegaptanib (P<0."( Pegaptanib for neovascular age-related macular degeneration.
Adamis, AP; Cunningham, ET; Feinsod, M; Gragoudas, ES; Guyer, DR, 2004
)
0.32
" No clear superiority of any particular dosage strength of pegaptanib was demonstrated, and no significant differences or trends favoured usual care on any domain score or the NEI-VFQ 25 composite score."( Quality of life in patients with age-related macular degeneration: results from the VISION study.
Leys, A; Patel, M; Shah, SN; Zlateva, G, 2008
)
0.35
" The pegaptanib dosing regimens were designed to achieve pegaptanib plasma concentrations of approximately 90, 270, or 900 ng/mL."( Local tolerance and systemic safety of pegaptanib sodium in the dog and rabbit.
Foy, JW; Modi, M; Patel, M; Rittenhouse, K, 2007
)
0.34
" Ongoing trials are evaluating the effectiveness of different dosing regimens, monitoring strategies, and combination therapies to determine the optimal niche for this new class of drugs in AMD management."( The evolving role of vascular endothelial growth factor inhibitors in the treatment of neovascular age-related macular degeneration.
Dadgostar, H; Waheed, N, 2008
)
0.35
" Studies are also needed to assess adverse events outside the proposed RCTs, to consider the optimal dosing regimes of these drugs and the benefits of re-treatment after initial treatment, and to review costing in more detail."( Ranibizumab and pegaptanib for the treatment of age-related macular degeneration: a systematic review and economic evaluation.
Clegg, AJ; Colquitt, JL; Jones, J; Price, A; Takeda, A; Tan, SC, 2008
)
0.35
" The time course and dose-response of photoreceptor cells in the rabbit retina after intravitreal injection of bevacizumab or pegaptanib sodium were examined by histologic analysis with hematoxylin and eosin (H&E) staining, caspase-3 and -9 immunostaining, and in situ terminal-deoxynucleotidyl transferase-mediated biotin-deoxyuridine triphosphate nick-end labeling (TUNEL) of DNA fragments of paraffin-embedded sections."( Comparative evaluation of apoptotic activity in photoreceptor cells after intravitreal injection of bevacizumab and pegaptanib sodium in rabbits.
Avci, B; Avci, R; Inan, UU; Kaderli, B, 2009
)
0.35
" A number of studies have shown that OCT imaging allows identification of functionally relevant factors like subretinal fluid or retinal thickness, which are important for the establishment of optimized individual dosing regimen during anti-angiogenesis therapies."( Antivascular endothelial growth factors in age-related macular degeneration.
Bolz, M; Mitsch, C; Pollreisz, A; Schmidt-Erfurth, U, 2010
)
0.36
"An intravitreal (IVT) ophthalmic dosing paradigm was designed based on clinical efficacy, nonclinical pharmacokinetics (PK), and disease progression modeling."( Integrating disease progression models, non-clinical pharmacokinetic data and treatment response endpoints to optimize intravitreal dosing regimens.
Amantea, M; Basile, AS; Johnson, TR; Klamerus, KJ; Nickens, DJ; Sultan, MB; Zhou, D, 2014
)
0.4
" Research evaluating variable dosing regimens with anti-VEGF agents, effects of long-term use, combination therapies (e."( Anti-vascular endothelial growth factor for neovascular age-related macular degeneration.
Hawkins, BS; Krzystolik, MG; Lindsley, K; Solomon, SD; Vedula, SS, 2014
)
0.4
" Future Cochrane Reviews should incorporate research evaluating variable dosing regimens of anti-VEGF agents, effects of long-term use, use of combination therapies (e."( Anti-vascular endothelial growth factor for neovascular age-related macular degeneration.
Hawkins, BS; Krzystolik, MG; Lindsley, K; Solomon, SD; Vedula, SS, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (397)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's195 (49.12)29.6817
2010's198 (49.87)24.3611
2020's4 (1.01)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials48 (10.48%)5.53%
Reviews145 (31.66%)6.00%
Case Studies50 (10.92%)4.05%
Observational1 (0.22%)0.25%
Other214 (46.72%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]