Pegaptanib

Identification

Summary

Pegaptanib is a selective vascular endothelial growth factor (VEGF) antagonist used for the treatment of neovascular (wet) age-related macular degeneration.

Generic Name
Pegaptanib
DrugBank Accession Number
DB04895
Background

Pegaptanib is a polynucleotide aptamer. Pegatinib aids neovascular age-related macular degeneration by binding to VEGF which in order reduces angiogenesis and vessel permeability.

Pegaptanib was granted FDA approval on 17 September 2004.5

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Nucleic Acid Based Therapies
Oligonucleotides
Synonyms
  • Pegaptanib Octasodium
  • Pegaptanib sodium
External IDs
  • EYE 001
  • NX 1838
  • NX1838

Pharmacology

Indication

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

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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

VEGF-A promotes angiogenesis.4 Patients with certain ocular conditions, such as the wet form of age related macular degeneration (AMD), have increased levels of VEGF-A.4,5 VEGF-A, in patients with wet AMD, also increases vascular permeability and inflammation in the eye, leading to progression of the condition.5 Pegaptanib is a pegylated oligonucleotide that selectively binds VEGF165, the isoform most responsible for VEGF-A's pathological action in wet AMD.5 This binding prevents VEGF165 from binding to its receptors, slowing or preventing further progression of wet AMD.5 Pegaptanib does not inhibit VEGF121, the physiological isoform.4

TargetActionsOrganism
AVascular endothelial growth factor A
antagonist
Humans
Absorption

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

Volume of distribution

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.

Protein binding

Not Available

Metabolism

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

Route of elimination

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.

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

Adverse Effects
Adverseeffects
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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.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Pegaptanib which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Pegaptanib which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Pegaptanib which could result in a higher serum level.
AcetaminophenAcetaminophen may decrease the excretion rate of Pegaptanib which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Pegaptanib which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Pegaptanib which could result in a higher serum level.
AclidiniumPegaptanib may decrease the excretion rate of Aclidinium which could result in a higher serum level.
AcrivastinePegaptanib may decrease the excretion rate of Acrivastine which could result in a higher serum level.
AcyclovirAcyclovir may decrease the excretion rate of Pegaptanib which could result in a higher serum level.
Adefovir dipivoxilAdefovir dipivoxil may decrease the excretion rate of Pegaptanib which could result in a higher serum level.
Interactions
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Food Interactions
No interactions found.

Products

Products2
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
MacugenSolution0.3 mg / 90 mcLIntravitrealPfizer Canada Ulc2005-08-262014-09-04Canada flag
MacugenInjection, solution0.3 mgIntravitrealPharma Swiss Ceska Republika S.R.O2016-09-082019-06-27EU flag
MacugenInjection, solution3.47 mg/1mLIntravitrealBausch Health US, LLC2004-12-172020-10-31US flag

Categories

ATC Codes
S01LA03 — Pegaptanib
Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
3HP012Q0FH
CAS number
222716-86-1

References

General References
  1. Vinores SA: Pegaptanib in the treatment of wet, age-related macular degeneration. Int J Nanomedicine. 2006;1(3):263-8. [Article]
  2. 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. [Article]
  3. 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 (Lond). 2009 Jan;23(1):181-5. Epub 2007 Aug 10. [Article]
  4. Shukla D, Namperumalsamy P, Goldbaum M, Cunningham ET Jr: Pegaptanib sodium for ocular vascular disease. Indian J Ophthalmol. 2007 Nov-Dec;55(6):427-30. doi: 10.4103/0301-4738.36476. [Article]
  5. FDA Approved Drug Products: Macugen (Pegaptanib) Intravitreous Injection [Link]
PubChem Substance
46504497
RxNav
498509
Therapeutic Targets Database
DAP001259
PharmGKB
PA164771236
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Pegaptanib
FDA label
Download (99.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedOtherAge - Related Macular Degeneration (AMD) / Diabetic Macular Edema (DME) / Retinal Vein Occlusion1
4CompletedTreatmentBranch Retinal Vein Occlusion1
4CompletedTreatmentDiabetic Macular Edema (DME)2
4CompletedTreatmentMacular Degeneration1
4RecruitingTreatmentMacular Diseases1
4TerminatedTreatmentAge - Related Macular Degeneration (AMD)1
4TerminatedTreatmentAge - Related Macular Degeneration (AMD) / Macular Degeneration / Subfoveal Choroidal Neovascularization (CNV)1
4TerminatedTreatmentMacular Degeneration1
4Unknown StatusTreatmentAge - Related Macular Degeneration (AMD)1
4Unknown StatusTreatmentProliferative Diabetic Retinopathy (PDR)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Eyetech Inc.
  • Gilead Sciences Inc.
  • Pfizer Inc.
Dosage Forms
FormRouteStrength
Injection, solutionIntravitreal
Injection, solutionIntravitreal0.3 mg
Injection, solutionIntravitreal3.47 mg/1mL
SolutionIntravitreal0.3 mg / 90 mcL
Prices
Unit descriptionCostUnit
Macugen 0.3 mg/0.09 ml1194.0USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6147204No2000-11-142010-06-11US flag
CA2269072No2006-02-142017-10-17Canada flag
US6011020No2000-01-042017-01-04US flag
US5932462No1999-08-032016-08-03US flag

Properties

State
Liquid
Experimental Properties
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Vascular endothelial growth factor receptor binding
Specific Function
Growth factor active in angiogenesis, vasculogenesis and endothelial cell growth. Induces endothelial cell proliferation, promotes cell migration, inhibits apoptosis and induces permeabilization of...
Gene Name
VEGFA
Uniprot ID
P15692
Uniprot Name
Vascular endothelial growth factor A
Molecular Weight
27042.205 Da
References
  1. Vinores SA: Pegaptanib in the treatment of wet, age-related macular degeneration. Int J Nanomedicine. 2006;1(3):263-8. [Article]
  2. Shukla D, Namperumalsamy P, Goldbaum M, Cunningham ET Jr: Pegaptanib sodium for ocular vascular disease. Indian J Ophthalmol. 2007 Nov-Dec;55(6):427-30. doi: 10.4103/0301-4738.36476. [Article]
  3. FDA Approved Drug Products: Macugen (Pegaptanib) Intravitreous Injection [Link]

Drug created on October 21, 2007 22:23 / Updated on April 30, 2021 13:06