DrugBank: Pegaptanib (DB04895)

targets (1)

Identification

Name

Pegaptanib

Accession Number

DB04895

Type

biotech

Groups

approved

Description

Pegaptanib is a pegylated anti-VEGF aptamer, a single strand of nucleic acid that binds with specificity to a particular target. 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]

Protein structure

Protein chemical formula

Not Available

Protein average weight

50000.0000

Sequences

Synonyms

Not Available

Synonyms

Not Available

Salts

Not Available

Brand names

Name	Company
Macugen

Brand mixtures

Not Available

Categories

Not Available

CAS number

222716-86-1

Taxonomy

Kingdom

Not Available

Classes

Not Available

Substructures

Not Available

Pharmacology

Indication

For the treatment of neovascular (wet) age-related macular degeneration.

Pharmacodynamics

Pegaptanib is a selective vascular endothelial growth factor (VEGF) antagonist. VEGF is a secreted protein that selectively binds and activates its receptors located primarily on the surface of vascular endothelial cells. VEGF induces angiogenesis, and increases vascular permeability and inflammation, all of which are thought to contribute to the progression of the neovascular (wet) form of age-related macular degeneration (AMD), a leading cause of blindness. VEGF has been implicated in blood retinal barrier breakdown and pathological ocular neovascularization.

Mechanism of action

Pegaptanib binds to the major pathological VEGF isoform, extracellular VEGF165, thereby inhibiting VEGF165 binding to its VEGF receptors. The inhibition of VEGF164, the rodent counterpart of human VEGF165, was effective at suppressing pathological neovascularization.

Absorption

In animals, pegaptanib is slowly absorbed into the systemic circulation from the eye after intravitreous administration.

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Based on preclinical data, pegaptanib is metabolized by endo- and exonucleases.

Route of elimination

Not Available

Half life

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.

Clearance

Not Available

Toxicity

Not Available

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacoeconomics

Manufacturers

Eyetech inc

Packagers

Dosage forms

Form	Route	Strength
Solution	Intravitreal

Prices

Unit description	Cost	Unit
Macugen 0.3 mg/0.09 ml	1194.0 USD	vial

Patents

Country	Patent Number	Approved	Expires (estimated)
United States	6011020	1997-01-04	2017-01-04
United States	6147204	1993-06-11	2010-06-11
Canada	2269072	2006-02-14	2017-10-17

Properties

State

liquid

Melting point

Not Available

Experimental Properties

Not Available

References

Synthesis Reference

Not Available

General Reference

Vinores SA: Pegaptanib in the treatment of wet, age-related macular degeneration. Int J Nanomedicine. 2006;1(3):263-8. Pubmed
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
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

External Links

Resource	Link
Drug Product Database	2267225
RxList	http://www.rxlist.com/cgi/generic/macugen.htm
Drugs.com	http://www.drugs.com/cdi/pegaptanib.html
Wikipedia	http://en.wikipedia.org/wiki/Pegaptanib

ATC Codes

Not Available

AHFS Codes

Not Available

PDB Entries

Not Available

FDA label

show (99.6 KB)

MSDS

Not Available

Interactions

Drug Interactions

Not Available

Food Interactions

Not Available

Targets
1. Neuropilin-1 Pharmacological action: unknown The soluble isoform 2 binds VEGF-165 and appears to inhibit its binding to cells. It may also induce apoptosis by sequestering VEGF-165. May bind as well various members of the semaphorin family. Its expression has an averse effect on blood vessel number and integrity Organism class: human UniProt ID: O14786 Gene: NRP1 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References: Vinores SA: Pegaptanib in the treatment of wet, age-related macular degeneration. Int J Nanomedicine. 2006;1(3):263-8. Pubmed

Targets

1. Neuropilin-1

Pharmacological action: unknown

The soluble isoform 2 binds VEGF-165 and appears to inhibit its binding to cells. It may also induce apoptosis by sequestering VEGF-165. May bind as well various members of the semaphorin family. Its expression has an averse effect on blood vessel number and integrity

Organism class: human
UniProt ID: O14786 Link_out

Gene: NRP1 Link_out

Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:

Vinores SA: Pegaptanib in the treatment of wet, age-related macular degeneration. Int J Nanomedicine. 2006;1(3):263-8. Pubmed

Comments

Drug created on October 21, 2007 16:23 / Updated on September 29, 2010 14:35