Selumetinib

Pronunciation: sel-ue-MET-i-nib
Generic name: selumetinib
Brand name: Koselugo
Dosage form: oral capsule (10 mg, 25 mg)
Drug class: Multikinase inhibitors

Medically reviewed by Carmen Pope, BPharm. Last updated on March 5, 2025.

What is selumetinib?

Selumetinib is used to treat neurofibromatosis type 1 (NF1) in children 2 years of age and older who have plexiform neurofibromas that cannot be completely removed by surgery. It is a capsule taken by mouth 2 times a day.

Selumetinib gained FDA approval on April 10, 2020 under the brand name Koselugo. There is no generic.

How does selumetinib work?

Selumetinib's mechanism of action involves blocking the action of 2 enzymes (MEK1 and 2) involved in signaling pathways for cell growth and division. Clinical trials have shown this reduces the number, volume, and spread of neurofibroma tumors.

Side effects

The most common side effects of selumetinib are:

• nausea, vomiting, stomach pain;

• itching;

• dry skin, acne, rash;

• redness around your fingernails;

• feeling weak or tired;

• mouth pain or soreness, swollen gums;

• muscle or bone pain;

• headache; or

• fever.

Diarrhea is a common side effect of this medicine. Tell your doctor right away the first time you have diarrhea while taking selumetinib.

Serious side effects and warnings

Selumetinib may cause the following serious side effects.

Heart problems. Clinical trials have shown selumetinib can lower the amount of blood pumped by your heart which is common and can also be severe. Your healthcare provider will do tests before and during treatment with selumetinib to check how well your heart is working. Tell your healthcare provider right away if you get any of the following signs or symptoms:

• persistent coughing or wheezing
• shortness of breath
• swelling of your ankles and feet
• tiredness
• increased heart rate.

Eye problems. Selumetinib can cause eye problems that can lead to blindness. Your healthcare provider will check your vision before and during treatment with selumetinib. Tell your healthcare provider right away if you get any of the following signs or symptoms:

• blurred vision
• loss of vision
• dark spots in your vision (floaters)
• other changes to your vision.

Severe diarrhea. Diarrhea is common with selumetinib and can also be severe. Tell your healthcare provider right away the first time that you get diarrhea during treatment with selumetinib. Your healthcare provider may give you medicine to help control your diarrhea and may tell you to drink more fluids.

Skin rash. Skin rashes are common with selumetinib and can also be severe. Tell your healthcare provider if you get any of the following signs or symptoms:

• rash that covers a large area of your body
• peeling skin
• blisters.

Muscle problems (rhabdomyolysis). Muscle problems are common with selumetinib and can also be severe. Treatment with selumetinib may increase the level of enzyme in your blood called creatine phosphokinase (CPK) and may be a sign of muscle damage. Your healthcare provider should do a blood test to check your blood levels of CPK before you start taking selumetinib and during treatment. Tell your healthcare provider right away if you get any of the following signs or symptoms:

• muscle aches or pain
• muscle spasms and weakness
• dark, reddish urine.

Drug interactions. Tell your healthcare provider if you are taking aspirin, blood thinners, or other medicines to treat blood clots. selumetinib contains vitamin E which may increase your risk of bleeding.

Your healthcare provider may change your dose, temporarily stop, or permanently ask you to stop taking selumetinib if you have any of these side effects.

These are not all of the possible side effects of selumetinib. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Related/similar drugs

Before taking

Before taking selumetinib, tell your healthcare provider about all of your medical conditions, including if you:

• have heart problems.
• have eye problems.
• have liver problems.
• are pregnant or plan to become pregnant
• are breastfeeding or plan to breastfeed.

selumetinib should not be given to a child younger than 2 years old.

Pregnancy

Selumetinib can harm an unborn baby. Your healthcare provider should check to see if you are pregnant before you begin treatment with selumetinib. Females who can become pregnant should use effective birth control (contraception) during treatment with selumetinib and for 1 week after their last dose.

Males with female partners who can become pregnant should use effective birth control (contraception) during treatment with selumetinib and for 1 week after their last dose.

Tell your healthcare provider right away if you become pregnant or think you may be pregnant during treatment with this treatment.

Breastfeeding

It is not known if selumetinib passes into your breast milk. Do not breastfeed during treatment with selumetinib and for 1 week after your last dose. Talk to your healthcare provider about the best way to feed your baby during this time.

How should I take selumetinib?

Take selumetinib exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets.

• Selumetinib is taken 2 times a day. Take each dose at the same time each day, about 12 hours apart.
• Take with a full glass of water.
• Swallow the capsule whole and do not crush, chew, break, or open it. Tell your doctor if your child has trouble swallowing the capsule whole.
• Selumetinib can be taken with or without food.

After taking

If you vomit shortly after taking selumetinib, do not take another dose. Wait until your next scheduled dose time to take the medicine again.

Tell your doctor if you start having loose stools. You may be given anti-diarrhea medicine. Keep using this medicine for as long as your doctor has prescribed.

• Drink plenty of liquids if you have diarrhea.

Selumetinib can cause your heart to pump less blood than normal. Your heart function will need to be checked every 3 to 6 months while you are taking this medicine.

Selumetinib can also cause eye problems that may lead to blindness. You will need frequent vision exams, and your next dose may be delayed based on the results.

Dosing information

Your healthcare provider will work out the correct dose based on your child's body surface area (height and weight). Your dose needs may change if you gain or lose weight or if you are still growing.

• Do not change your dose or dosing schedule without your doctor's advice.

Usual child 2 years and older dose for NF1:

• Selumetinib 25 mg/m² orally 2 times a day (approximately every 12 hours) until disease progression or unacceptable toxicity

Reduce the recommended dosage to 20 mg/m² orally 2 times a day for patients with moderate hepatic impairment (Child-Pugh B).

• The dosage for use in patients with severe hepatic impairment (Child-Pugh C) has not been established.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if your next dose is due in less than 6 hours. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What to avoid

Do not drink grapefruit juice, eat grapefruit or take supplements that contain grapefruit or St. John's wort during treatment with selumetinib.

What other drugs will affect selumetinib?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, or herbal supplements. Especially tell your healthcare provider if you are taking aspirin, blood thinners, or other medicines to treat blood clots. selumetinib contains vitamin E which may increase your risk of bleeding.

Storage

Store selumetinib at room temperature away from moisture and heat. Keep the capsules in their original container, along with the packet or canister of moisture-absorbing preservative.

Manufacturer

AstraZeneca, a British-Swedish pharmaceutical company headquartered in Cambridge, UK, makes selumetinib under the brand name Koselugo. Some of AstraZeneca's other notable drugs include:

• Tagrisso (osimertinib) for lung cancer
• Calquence (acalabrutinib) for blood cancers
• Lynparza (olaparib) for various cancers
• Farxiga (dapagliflozin) for diabetes and heart failure
• Symbicort (budesonide/formoterol) for asthma and COPD.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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