Koselugo

Pronunciation: ko-SEL-u-go
Generic name: selumetinib
Dosage form: oral capsule (10 mg, 25 mg)
Drug class: Multikinase inhibitors 

What is Koselugo?

Koselugo is used to treat neurofibromatosis type 1 (NF1) in children aged 2 and older with plexiform neurofibromas that cannot be completely removed by surgery. It is an oral capsule that is taken 2 times a day.

Koselugo (selumetinib) gained FDA approval on April 10, 2020. There is no generic.

How does Koselugo work?

Koselugo’s mechanism of action involves blocking the actions of 2 enzymes, MEK1 and 2. These proteins are critical components of signalling pathways involved in cell growth and division. Clinical trials have shown this medication reduces the number, volume, and spread of neurofibroma tumors.

Koselugo (selumetinib)  belongs to the drug class called multikinase inhibitors.

Side effects

The most common side effects of Koselugo 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 Koselugo.

Serious side effects and warnings

Koselugo may cause the following serious side effects:

• Heart problems. Clinical trials have shown that Koselugo 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 Koselugo 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. Koselugo can cause eye problems that can lead to blindness. Your healthcare provider will check your vision before and during treatment with Koselugo. 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 Koselugo and can also be severe. Tell your healthcare provider right away the first time that you get diarrhea during treatment with Koselugo. 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 Koselugo and can also be severe. Tell your healthcare provider if you get any of the following signs or symptoms:
  • a rash that covers a large area of your body
  • peeling skin
  • blisters.
• Muscle problems (rhabdomyolysis). Muscle problems are common with Koselugo and can also be severe. Treatment with Koselugo may increase levels of an enzyme in your blood called creatine phosphokinase (CPK) which 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 Koselugo 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 take aspirin, blood thinners, or other medicines to treat blood clots. Koselugo 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 Koselugo if you have any of these side effects.

These are not all of the possible side effects of Koselugo. Call your doctor for medical advice about side effects. You may report side effects to the FDA .

Before taking

Before taking Koselugo, 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.

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

Pregnancy

Koselugo can harm an unborn baby. Your healthcare provider should check to see if you are pregnant before you begin treatment with Koselugo. Females who can become pregnant should use effective birth control (contraception) during treatment with Koselugo 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 Koselugo 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 medication.

Breastfeeding

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

How should I take Koselugo?

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

• Koselugo is a capsule that is taken 2 times a day.
• Can be taken with or without food.
• 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.

After taking

If you vomit shortly after taking Koselugo, 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 (diarrhea). 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.

Koselugo 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.

Koselugo 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 decides the correct dose for you based on 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 dose for children 2 years and older for NF1:

• Koselugo 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.