U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
Pegaptanib is a selective vascular endothelial growth factor (VEGF) antagonist indicated for the treatment of neovascular (wet) age-related macular degeneration. Pegaptanib is an aptamer, a pegylated modified single-stranded oligonucleotide, which adopts a threedimensional conformation that enables it to bind to extracellular VEGF. Pegaptanib specifically binds to the 165 isoform of VEGF, 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 age-related macular degeneration. Pegaptanib is administered in a 0.3 mg dose once every six weeks by intravitreal injection. An intravitreal injection is one that is administered directly into the eye, more specifically, into the vitreous humour, or the jelly-like fluid within the eye.

Approval Year

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
PubMed

PubMed

TitleDatePubMed
Resolution of persistent exudative retinal detachment in a case of Sturge-Weber syndrome with anti-VEGF administration.
2009 Jul-Aug

Sample Use Guides

Pegaptanib 0.3 mg should be administered once every six weeks by intravitreous injection into the eye to be treated.
Route of Administration: Other
Substance Class Nucleic Acid
Created
by admin
on Sat Dec 16 15:52:44 GMT 2023
Edited
by admin
on Sat Dec 16 15:52:44 GMT 2023
Nucleic Acid Type OLIGONUCLEOTIDE
Nucleic Acid Subtype
Record UNII
2H1PA8H1EN
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PEGAPTANIB
EMA EPAR   INN   VANDF   WHO-DD  
INN  
Official Name English
PEGAPTANIB [EMA EPAR]
Common Name English
pegaptanib [INN]
Common Name English
Pegaptanib [WHO-DD]
Common Name English
PEGAPTANIB [VANDF]
Common Name English
Classification Tree Code System Code
WHO-VATC QS01LA03
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
NCI_THESAURUS C1742
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
NDF-RT N0000178292
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
WHO-ATC S01LA03
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
EMA ASSESSMENT REPORTS MACUGEN (AUTHORIZED: WET MACULAR DEGENERATION)
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
Code System Code Type Description
NCI_THESAURUS
C90657
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY
NDF-RT
N0000170810
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY Aptamers, Nucleotide [Chemical/Ingredient]
INN
8215
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY
RXCUI
498509
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY RxNorm
NDF-RT
N0000011393
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY Oligonucleotides [Chemical/Ingredient]
ChEMBL
CHEMBL2108752
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY
IUPHAR
6836
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY
DRUG BANK
DB04895
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY
MESH
C495058
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY
WIKIPEDIA
PEGAPTANIB
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY
DRUG CENTRAL
4905
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY
EVMPD
SUB25196
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY
FDA UNII
2H1PA8H1EN
Created by admin on Sat Dec 16 15:52:44 GMT 2023 , Edited by admin on Sat Dec 16 15:52:44 GMT 2023
PRIMARY
Sugar Site Range Site Count
D-Ribose (RNA) 1_4-1_5 2 / 28
Deoxyribose (DNA) 1_28 1 / 28
2'-O-Methyl-Ribose 1_2-1_3;1_8-1_9;1_11-1_13;1_15;1_19;1_21;1_23;1_27 12 / 28
2'-Fluoro-Ribose 1_1;1_6-1_7;1_10;1_14;1_16-1_18;1_20;1_22;1_24-1_26 13 / 28
Linkage Site Range Site Count
Phosphate 1_1-1_27 27 / 27
Related Record Type Details
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY

Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
NUCLEOTIDE SUBSTITUTION [1_28] THYMIDINE 3'-MONOPHOSPHATE Q84LAH3NDH
PEGYLATION [1_1] SITE_SPECIFIC PEGAPTANIB, PEGYLATED 2'-DEOXY-2'-FLUOROURIDINE 5'-MONOPHOSPHATE- 0E3EGS14RZ