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Class: EENT Drugs, Miscellaneous
VA Class: OP900
Molecular Formula: C294H342F13N107Na28O188P28[C2H4O]n where n is approximately 900.
CAS Number: CAS-222716-86-1
Brands: Macugen

Medically reviewed by Last updated on May 22, 2020.


Polyethylene glycol (PEG)-conjugated, modified synthetic RNA oligonucleotide and aptamer; selective vascular endothelial growth factor (VEGF) antagonist.1 3 13 14 15 16

Uses for Pegaptanib

Neovascular Age-related Macular Degeneration

Treatment of neovascular (wet) age-related macular degeneration.1 2 6 9 13 14 15 16 17

Pegaptanib Dosage and Administration


  • Manufacturer’s prescribing information should be consulted for details on assembly and proper use of the syringes.1


Ophthalmic Administration

Evaluate patient’s medical history for hypersensitivity reactions to prior intravitreal administration of the drug.1 19 (See Contraindications and also see Hypersensitivity Reactions under Cautions.)

Administer by intravitreal injection only into a single affected eye.1 2 9 14 16 Safety and efficacy of treating both eyes concurrently not determined.1 14

Pegaptanib injection does not need to reach room temperature prior to administration.14

Inject following adequate anesthesia and administration of broad-spectrum anti-infective agents.1 2 4 9 14 15 18

Inject under controlled aseptic conditions (including use of sterile gloves, sterile drape, a sterile eyelid speculum [or equivalent]).1 2 4 9 14 15 18

Monitor patients for elevation of intraocular pressure (IOP) and for development of endophthalmitis following intravitreal injection.1 18

Monitoring for IOP may include evaluation of optic nerve head perfusion immediately after the injection, tonometry within 30 minutes following the injection, and biomicroscopy between 2 and 7 days following injection.1 2 18


Available as pegaptanib sodium; dosage expressed in terms of the free acid of the oligonucleotide without polyethylene glycol.1 13 14


Neovascular Age-related Macular Degeneration
Ophthalmic Administration

Intravitreal injection: 0.3 mg into the affected eye every 6 weeks.1 2

Doses exceeding 0.3 mg do not appear to provide additional therapeutic benefit;1 2 14 15 doses exceeding 1 mg have been associated with decreased efficacy.1

Safety and efficacy of pegaptanib beyond 2 years of therapy have not been established.1

Special Populations

Renal Impairment

No dosage adjustment required.1

Cautions for Pegaptanib


  • Ocular or periocular infections.1 18

  • Known hypersensitivity to pegaptanib or any ingredient in the formulation.1 19



Endophthalmitis and Other Serious Ocular Effects

Intravitreal injections of pegaptanib associated with endophthalmitis.1 2 13 15 18

Monitor patients closely for signs of endophthalmitis (e.g., redness, sensitivity to light, pain, changes in vision) during the week following injection to permit early treatment.1 2 18

The most common isolate cultured in patients with endophthalmitis after receiving pegaptanib was coagulase-negative Staphylococcus epidermiditis.2

Proper aseptic injection technique should be used to decrease potential for infection.1 2 15 18 (See Ophthalmic Administration under Dosage and Administration.)

Risk of retinal detachment and iatrogenic traumatic cataract.1

Increased IOP

Risk of increased IOP within 30 minutes of intravitreal injection.1

Monitor and manage appropriately IOP and optic nerve head perfusion.1 19 (See Ophthalmic Administration under Dosage and Administration.)

Sensitivity Reactions

Hypersensitivity Reactions

Rare cases of anaphylaxis/anaphylactoid reactions, including angioedema, reported following intravitreal administration procedure with pegaptanib.1 19

Evaluate patient’s medical history for hypersensitivity reactions prior to intravitreal administration of the drug.1 19

Specific Populations


Category B.1


Not known whether pegaptanib is distributed into milk.1 Caution advised if intravitreal injection is used.1

Pediatric Use

Safety and efficacy not established in children.1 14

Adult Use

Safety and efficacy not established in adults <50 years of age.14

Geriatric Use

No substantial differences in efficacy or systemic exposure relative to younger adults.1

Hepatic Impairment

Pharmacokinetics not studied in patients with hepatic impairment.1

Renal Impairment

No dosage adjustment required in patients with renal impairment.1 Not evaluated in patients undergoing hemodialysis.1

Common Adverse Effects

Anterior chamber inflammation,1 2 blurred vision,1 cataract,1 conjunctival hemorrhage,1 corneal edema,1 2 eye discharge,1 2 eye irritation,1 eye pain,1 2 hypertension,1 increased IOP,1 ocular discomfort,1 punctuate keratitis,1 2 vitreous floaters or opacities,1 2 reduced visual acuity,1 visual disturbance.1

Interactions for Pegaptanib

No formal drug interaction studies to date.1

Metabolized by nucleases; generally not affected by CYP isoenzymes.1

Photodynamic Therapy with Verteporfin

No apparent difference in the pharmacokinetic profile of pegaptanib involving patients treated with pegaptanib alone or in combination with photodynamic therapy and verteporfin.1 9 14 No adverse effects attributed directly to concomitant use of pegaptanib with verteporfin.2 4

Pegaptanib Pharmacokinetics



Slowly absorbed into systemic circulation from the eye with mean peak plasma concentration usually attained within 1–4 days.1



Distributed into vitreous fluid, retina, aqueous fluid, and kidneys.1

Crosses the placenta in mice; not known whether crosses the placenta in humans.1

Not known whether distributed into human milk.1



Appears to be metabolized by endo- and exonucleases.1

Elimination Route

In animals, excreted principally in urine as unchanged drug and metabolites.1


Average: 10 days.1

Special Populations

No dosage adjustment required in those with renal impairment.1




2–8°C; do not freeze or shake vigorously.1

May be kept at room temperature for up to 8 hours.14


  • Binds to extracellular VEGF165, the major VEGF isoform involved in the pathogenesis of the neovascular (wet) form of age-related macular degeneration and inhibits VEGF165 from binding to VEGF receptors.1 2 3 7 8 9 10 11 12 13 14 15 16

  • VEGF induces angiogenesis and increases vascular permeability and inflammation, all of which appear to play a role in the pathogenesis of neovascular age-related macular degeneration, a leading cause of blindness in adults >55 years of age in developed countries.1 2 3 5 6 7 8 9 10 11 12 13 15 The neovascular form of the disease represents about 10% of overall disease prevalence, but it is responsible for 90% of severe vision loss.2

Advice to Patients

  • Necessity of advising patients about the risk of developing endophthalmitis.1 Importance of informing their ophthalmologist immediately if changes in vision occur or the treated eye becomes red, sensitive to light, or painful.1

  • Patients should be instructed to immediately report any symptoms suggestive of endophthalmitis.1 2 18 (See Endophthalmitis and Other Serious Ocular Effects under Cautions.)

  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1

  • Importance of informing patients of other important precautionary information. (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Pegaptanib Sodium


Dosage Forms


Brand Names



Injection, for intravitreal use only

0.3 mg/0.09 mL (of the free acid of the oligonucleotide without polyethylene glycol)

Macugen (preservative-free; available as single-dose prefilled syringe with needle)

Eyetech (also promoted by Pfizer)

AHFS DI Essentials™. © Copyright 2021, Selected Revisions June 1, 2007. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.


1. Eyetech. Macugen (pegaptanib sodium) injection prescribing information. New York, NY; 2006 Apr.

2. Gragoudas ES, Adamis AP, Cunningham ET Jr et al. Pegaptanib for neovascular age-related macular degeneration. N Engl J Med. 2004; 351:2805-16.

3. Vinores SA. Technology evaluation: pegaptanib, Eyetech/Pfizer. Curr Opin Mol Ther. 2003; 5:673-9.

4. Supplementary appendix to: Gragoudas ES, Adamis AP, Cunningham ET Jr et al. Pegaptanib for neovascular age-related macular degeneration. N Engl J Med. 2004; 351:2805-16. From the New England Journal of Medicine website ( Accessed 2005 Mar 21.

5. Congdon N, O’Colmain B, Klaver CC et al. Causes and prevalence of visual impairment among adults in the United States. Arch Ophthalmol. 2004 Apr; 122:477-85.

6. Ferris FL 3rd. A new treatment for ocular neovascularization. N Engl J Med. 2004; 351:2863-5.

7. Nimjee SM, Rusconi CP, Sullenger BA. Aptamers: an emerging class of therapeutics. Annu Rev Med. 2005; 56:555-83.

8. The Eyetech Study Group. Preclinical and phase 1A clinical evaluation of an anti-VEGF pegylated aptamer (EYE001) for the treatment of exudative age-related macular degeneration. Retina. 2002; 22:143-52.

9. The Eyetech Study Group. Anti-vascular endothelial growth factor therapy for subfoveal choroidal neovascularization secondary to age-related macular degeneration: phase II study results. Ophthalmology. 2003; 110:979-86.

10. Csaky K. Anti-vascular endothelial growth factor therapy for neovascular age-related macular degeneration: promises and pitfalls. Ophthalmology. 2003; 110:879-81. Guest Editorial.

11. Frank RN. Diabetic retinopathy. N Engl J Med. 2004; 350:48-58.

12. Aiello LP, Avery RL, Arrigg PG et al. Vascular endothelial growth factor in ocular fluid of patients with diabetic retinopathy and other retinal disorders. N Engl J Med. 1994; 331:1480-7.

13. Siddiqui MAA, Keating GM. Pegaptanib: in exudative age-related macular degeneration. Drugs. 2005; 65:1571-7.

14. Pfizer, Morris Plains, NJ: Personal communication.

15. van Wijngaarden P, Coster DJ, Williams KA. Inhibitors of ocular neovascularization: promises and potential problems. JAMA. 2005; 293:1509-13.

16. Anon. Pegaptanib sodium (Macugen) for macular degeneration. Med Lett Drugs Ther. 2005; 47:55-6.

17. D’Amico DJ for the VEGF Inhibition Study in Ocular Neovascularization (VISION) Clinical Trial Group. VEGF inhibition study in ocular neovascularization (VISION): second year efficacy data. Invest Ophthalmol Vis Sci. 2005; 46: E-Abstract 2309.

18. Aiello LP, Brucker AJ, Chang S et al. Evolving guidelines for intravitreous injections. Retina. 2004; 24:S3-19.

19. Dear health care provider letter regarding rare reports of anaphylaxis/anaphylactoid reactions, including angioedema following administration of Macugen with other drugs as part of the injection preparation procedure. New York, NY: Eyetech and Pfizer; 2006 March 6.