Pegaptanib

What is pegaptanib used for?

Pegaptanib is a prescription medicine that is used to treat macular degeneration.

Description

Macugen (pegaptanib sodium injection) is a sterile, aqueous solution containing pegaptanib sodium for intravitreous injection. Macugen is supplied in a single-dose, pre-filled syringe and is formulated as a 3.47 mg/mL solution, measured as the free acid form of the oligonucleotide. The active ingredient is 0.3 mg of the free acid form of the oligonucleotide without polyethylene glycol, in a nominal volume of 90 μL. This dose is equivalent to 1.6 mg of pegaptanib sodium (pegylated oligonucleotide) or 0.32 mg when expressed as the sodium salt form of the oligonucleotide moiety. The product is a sterile, clear, preservative-free solution containing sodium chloride, monobasic sodium phosphate monohydrate, dibasic sodium phosphate heptahydrate, hydrochloric acid, and/or sodium hydroxide to adjust the pH and water for injection.

Pegaptanib sodium is a covalent conjugate of an oligonucleotide of twenty-eight nucleotides in length that terminates in a pentylamino linker, to which two 20-kilodalton monomethoxy polyethylene glycol (PEG) units are covalently attached via the two amino groups on a lysine residue.

Pegaptanib sodium is represented by the following structural formula:

 

 

Where R is

 

 

and n is approximately 450.

The chemical name for pegaptanib sodium is as follows: RNA, ((2′-deoxy-2′-fluoro)C-G_m-G_m-A-A-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)C-A_m-G_m-(2′-deoxy-2′-fluoro)U-G_m-A_m-A_m-(2′-deoxy-2′-fluoro)U-G_m-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2’fluoro)U-A_m-(2′-deoxy-2′-fluoro)U-A_m-(2′-deoxy-2′-fluoro)C-A_m-(2′-deoxy-2′-fluoro)U-(2’deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)C-G_m-(3’→3′)-dT), 5′-ester with α,α’-[4,12-dioxo-6[[[5-(phosphoonoxy)pentyl]amino] carbonyl]-3,13-dioxa-5,11-diaza-1,15pentadecanediyl]bis[ω-methoxypoly(oxy-1,2-ethanediyl)], sodium salt.

The molecular formula for pegaptanib sodium is C₂₉₄H₃₄₂F₁₃N₁₀₇Na₂₈O₁₈₈P₂₈[C₂H₄O]_n (where n is approximately 900) and the molecular weight is approximately 50 kilodaltons.

Macugen is formulated to have an osmolality of 280-360 mOsm/Kg, and a pH of 6–7.

Before taking pegaptanib, tell your doctor:

• If you are allergic to pegaptanib; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
• If you have an infection in or around the eye.

This is not a list of all drugs or health problems that interact with pegaptanib.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take pegaptanib with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take pegaptanib?

• Tell all of your health care providers that you take pegaptanib. This includes your doctors, nurses, pharmacists, and dentists.
• Use care when driving or doing other tasks that call for clear eyesight.
• Have your eye pressure checked. Talk with your doctor.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using pegaptanib while you are pregnant.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

How is pegaptanib best taken?

Use pegaptanib as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• It is given as a shot into the eye.

What do I do if I miss a dose?

• Call your doctor to find out what to do.

What are the side effects of pegaptanib that I need to call my doctor about immediately?

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Very bad headache.
• Change in eyesight, eye pain, or very bad eye irritation.
• Trouble passing urine.
• Pain when passing urine.
• Eyelid swelling.
• Eye redness.
• Eye discharge.
• Bleeding in the eye.
• Eye is bothered by bright light.

What are some other side effects of pegaptanib?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Eye irritation.
• Seeing floaters.
• Dizziness.
• Diarrhea.
• Headache.
• Upset stomach.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out pegaptanib?

• If you need to store pegaptanib at home, talk with your doctor, nurse, or pharmacist about how to store it.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.

SRC: NLM .