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.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Neovascular age-related macular degeneration •••••••••••• - Contraindications & Blackbox Warnings
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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
Target Actions Organism AVascular endothelial growth factor A antagonistHumans - 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
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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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Pegaptanib which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Pegaptanib which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Pegaptanib which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Pegaptanib which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Pegaptanib which could result in a lower serum level and potentially a reduction in efficacy. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Macugen Solution 0.3 mg / 90 mcL Intravitreal Pfizer Canada Ulc 2005-08-26 2014-09-04 Canada 
Macugen Injection, solution 3.47 mg/1mL Intravitreal Bausch Health US, LLC 2004-12-17 2020-10-31 US 
Macugen Injection, solution 0.3 mg Intravitreal Pharma Swiss Ceska Republika S.R.O 2016-09-08 2022-12-02 EU 
Categories
- ATC Codes
- S01LA03 — Pegaptanib
- Drug Categories
- Antineovascularisation Agents
- Carbohydrates
- Drugs that are Mainly Renally Excreted
- Glycosides
- Nucleic Acids, Nucleotides, and Nucleosides
- Nucleotides
- Ocular Vascular Disorder Agents
- Oligonucleotides
- Ophthalmologicals
- Pegylated agents
- Polynucleotides
- Sensory Organs
- Vascular Endothelial Growth Factor A
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 3HP012Q0FH
- CAS number
- 222716-86-1
References
- General References
- Vinores SA: Pegaptanib in the treatment of wet, age-related macular degeneration. Int J Nanomedicine. 2006;1(3):263-8. [Article]
- 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]
- 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]
- 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]
- FDA Approved Drug Products: Macugen (Pegaptanib) Intravitreous Injection [Link]
- External Links
- PubChem Substance
- 46504497
- 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
Phase Status Purpose Conditions Count 4 Completed Other Age - Related Macular Degeneration (AMD) / Diabetic Macular Edema (DME) / Retinal Vein Occlusion 1 4 Completed Treatment Branch Retinal Vein Occlusion 1 4 Completed Treatment Diabetic Macular Edema (DME) 2 4 Completed Treatment Macular Degeneration 1 4 Recruiting Treatment Macular Diseases 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Eyetech Inc.
- Gilead Sciences Inc.
- Pfizer Inc.
- Dosage Forms
Form Route Strength Injection, solution Intravitreal Injection, solution Intravitreal 0.3 mg Injection, solution Intravitreal 3.47 mg/1mL Solution Intravitreal 0.3 mg / 90 mcL - Prices
Unit description Cost Unit Macugen 0.3 mg/0.09 ml 1194.0USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6147204 No 2000-11-14 2010-06-11 US CA2269072 No 2006-02-14 2017-10-17 Canada US6011020 No 2000-01-04 2017-01-04 US US5932462 No 1999-08-03 2016-08-03 US
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- 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
- Vinores SA: Pegaptanib in the treatment of wet, age-related macular degeneration. Int J Nanomedicine. 2006;1(3):263-8. [Article]
- 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]
- FDA Approved Drug Products: Macugen (Pegaptanib) Intravitreous Injection [Link]
Drug created at October 21, 2007 22:23 / Updated at December 04, 2021 06:47