Selumetinib

What is Selumetinib?

• Selumetinib (Koselugo) is a kinase inhibitor used to treat children 2 years of age and older with neurofibromatosis type 1 (NF1).

What are the uses of this medicine?

• This medicine is indicated for the treatment of pediatric patients 2 years of age and older with neurofibromatosis type 1 (NF1) who have plexiform neurofibromas that cannot be completely removed by surgery.

How does this medicine work?

• (SEL-yoo-MEH-tih-nib) A substance being studied in the treatment of several types of cancer.
• Selumetinib blocks proteins needed for cell growth and may kill cancer cells.
• It is a type of protein kinase inhibitor.
• Also called AZD6244 and MEK inhibitor AZD6244.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

Avoid concomitant use with :

• Strong or Moderate CYP3A4 Inhibitors or Fluconazole
• Strong or Moderate CYP3A4 Inducers

Is this medicine FDA approved?

• It was approved for use in the United States in 2020.

How should this medicine be used?

Recommended Dosage

• The recommended dosage of Koselugo is 25 mg/m2 orally twice daily (approximately every 12 hours) until disease progression or unacceptable toxicity.
• Reduce the recommended dosage to 20 mg/m2 orally twice daily for patients with moderate hepatic impairment (Child-Pugh B).
• The recommended dosage for use in patients with severe hepatic impairment (Child-Pugh C) has not been established.

Administration

• Take Koselugo exactly as your healthcare provider tells you to.
• Do not change your dose or stop taking Koselugo unless your healthcare provider tells you to.
• Your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with Koselugo if you have side effects.
• Your healthcare provider will decide on the right dose of Koselugo based on your weight or size (body surface area) and how many capsules of Koselugo to take.
• Koselugo should be taken around the same time each day, about 12 hours apart.
• Take Koselugo on an empty stomach. Do not eat food for 2 hours before your dose and 1 hour after your dose.
• Swallow Koselugo capsules whole with water. Do not chew, dissolve, or open the capsules.
• If you miss a dose of Koselugo, take it as soon as you remember. If it is less than 6 hours before your next scheduled dose, take your next dose at your regular time. Do not make up for the missed dose.
• If you vomit at any time after taking Koselugo, do not take an additional dose. Take your next dose at your regular time.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 10 mg and 25 mg

This medicine is available in fallowing brand namesː

• Koselugo

What side effects can this medication cause?

Common possible side effects and laboratory abnormalities of this medicine include:

• vomiting
• stomach pain
• nausea
• dry skin
• feeling of tiredness, weakness or lacking energy
• muscle and bone pain
• fever
• inflammation of the mouth
• headache
• redness around the fingernails
• itching

Koselugo may cause serious side effects, including:

• Heart Problems
• Eye Problems
• Severe diarrhea
• Skin Rash
• Muscle problems (rhabdomyolysis)

What special precautions should I follow?

• Conduct ophthalmic assessments prior to initiating Koselugo, at regular intervals during treatment and for new or worsening visual changes.
• Advise patients to start an anti-diarrheal agent immediately after the first episode of loose stool and to increase fluid intake. Withhold, reduce dose, or permanently discontinue Koselugo based on severity of adverse reaction.
• Monitor for severe skin rashes. Withhold, reduce dose, or permanently discontinue Koselugo based on severity of adverse reaction.
• Increased CPK and rhabdomyolysis can occur. Obtain serum CPK prior to initiating Koselugo, periodically during treatment, and as clinically indicated. Withhold, reduce dose, or permanently discontinue Koselugo based on severity of adverse reaction.
• Koselugo capsules contain vitamin E and daily intake of vitamin E that exceeds the recommended or safe limits may increase the risk of bleeding. An increased risk of bleeding may occur in patients coadministered vitamin-K antagonists or anti-platelet agents.
• Assess ejection fraction prior to initiating treatment, every 3 months during the first year, then every 6 months thereafter and as clinically indicated.

What to do in case of emergency/overdose?

• Dialysis is not helpful as Koselugo is highly protein bound and is extensively metabolized.

Can this medicine be used in pregnancy?

• Koselugo can cause fetal harm when administered to a pregnant woman.
• There are no available data on the use of Koselugo in pregnant women to evaluate drug-associated risk.

Can this medicine be used in children?

• The safety and effectiveness have been established in pediatric patients 2 years of age and older with NF1 who have inoperable PN.
• The safety and effectiveness of Koselugo have not been established in pediatric patients younger than 2 years of age.

What are the active and inactive ingredients in this medicine?

Active ingredient: selumetinib.

Inactive ingredients: Capsule contains: vitamin E polyethylene glycol succinate.

• The 10 mg capsule shell contains: hypromellose, carrageenan, potassium chloride, titanium dioxide, carnauba wax, and purified water.
• The 10 mg capsule printing ink contains: shellac, iron oxide black, propylene glycol, and ammonium hydroxide.
• The 25 mg capsule shell contains: hypromellose, carrageenan, potassium chloride, titanium dioxide, FD&C blue 2, ferric oxide yellow, purified water, carnauba wax and/or corn starch.

• The 25 mg printing ink contains: ferric oxide red, ferric oxide yellow, FD&C Blue 2 aluminum lake, carnauba wax, shellac, glyceryl monooleate.

Who manufactures and distributes this medicine?

• Distributed by: AstraZeneca Pharmaceuticals LP, Wilmington, DE

What should I know about storage and disposal of this medication?

• Store Koselugo at room temperature, between 68°F to 77°F (20°C to 25°C).
• The bottle of Koselugo contains a desiccant packet to reduce moisture. Do not throw away desiccant packet.
• Keep Koselugo in its original bottle.

• Dailymed label info on Selumetinib
• FDA Selumetinib

Selumetinib Resources
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