Belumosudil

What is Belumosudil?

• Belumosudil (Rezurock) is a kinase inhibitor used to treat chronic graft-versus-host disease after failure of at least two prior lines of systemic therapy.

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Belumosudil - KD025

What are the uses of this medicine?

• Belumosudil (Rezurock) is a prescription medicine used to treat adults and children 12 years of age and older with chronic graft-versus-host disease (chronic GVHD) after you have received at least 2 prior treatments (systemic therapy) and they did not work.

How does this medicine work?

• It is in the class of drugs known as serine/threonine kinase inhibitors.
• Belumosudil is an inhibitor of rho-associated, coiled-coil containing protein kinase (ROCK) which inhibits ROCK2 and ROCK1.
• Belumosudil binds to and inhibits the serine/threonine kinase activity of ROCK2.
• This inhibits ROCK2-mediated signaling pathways which play major roles in pro- and anti-inflammatory immune cell responses.
• Belumosudil down-regulated proinflammatory responses via regulation of STAT3/STAT5 phosphorylation and shifting Th17/Treg balance.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Rezurock may affect the way other medicines work, and other medicines may affect the way Rezurock works.
• Coadministration of Rezurock with strong CYP3A inducers decreases belumosudil exposure, which may reduce the efficacy of Rezurock. Increase Rezurock dosage to 200 mg twice daily.
• Coadministration of Rezurock with proton pump inhibitors decreases belumosudil exposure , which may reduce the efficacy of Rezurock. Increase Rezurock dosage to 200 mg twice daily.

Is this medicine FDA approved?

• Belumosudil was approved for medical use in the United States in July 2021.

How should this medicine be used?

Recommended dosage:

• The recommended dose of Rezurock is 200 mg given orally once daily until progression of chronic GVHD that requires new systemic therapy.

Administration:

• Take Rezurock 1 time a day with a meal.
• Take Rezurock at about the same time each day.
• Swallow Rezurock tablets whole with a glass of water.
• Do not cut, crush, or chew Rezurock tablets.
• Your healthcare provider will do blood tests to check your liver at least 1 time a month during treatment with Rezurock.
• If you miss a dose of Rezurock, take it as soon as you remember on the same day. Take your next dose of Rezurock at your regular time on the next day. Do not take extra doses of Rezurock to make up for a missed dose.
• If you take too much Rezurock, call your healthcare provider or go to the nearest hospital emergency room right away.

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

This medicine is available in fallowing doasage form:

• As Tablet: 200 mg.

This medicine is available in fallowing brand namesː

• Rezurock

What side effects can this medication cause?

The most common side effects of this medicine include:

• infections
• tiredness or weakness
• nausea
• diarrhea
• shortness of breath
• cough
• swelling
• bleeding
• stomach (abdominal) pain
• muscle or bone pain
• headache
• high blood pressure

What special precautions should I follow?

• Based on findings in animals and its mechanism of action, Rezurock can cause fetal harm when administered to a pregnant woman.
• Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to inform their healthcare provider of a known or suspected pregnancy.
• Advise females of reproductive potential to use effective contraceptive during treatment with Rezurock and for at least one week after the last dose.
• Advise males with female partners of reproductive potential to use effective contraceptive during treatment with Rezurock and for at least one week after the last dose.
• Advise women not to breastfeed during treatment with Rezurock and for at least one week after the last dose.
• Advise males and females of reproductive potential that Rezurock may impair fertility.
• Advise patients to inform their health care providers of all concomitant medications, including prescription medicines, over-the-counter drugs, vitamins, and herbal products.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Rezurock can cause fetal harm when administered to pregnant women.
• Females who can become pregnant should use effective birth control during treatment with Rezurock and for at least 1 week after the last dose.
• Males with female partners who can become pregnant should use effective birth control during treatment with Rezurock and for at least 1 week after the last dose.

Can this medicine be used in children?

• It is not known if Rezurock is safe and effective in children less than 12 years old.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• belumosudil mesylate

Inactive ingredients:

• Tablet core: microcrystalline cellulose, hypromellose, croscarmellose sodium, colloidal silicon dioxide, and magnesium stearate.
• Tablet coating: polyvinyl alcohol, polyethylene glycol, talc, titanium dioxide and yellow iron oxide.

Who manufactures and distributes this medicine?

• Distributed and marketed by Kadmon Pharmaceuticals, LLC, Warrendale, PA
• Rezurock™ is a trademark of Kadmon Pharmaceuticals, LLC

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

• Store at room temperature, 20°C to 25°C (68°F to 77°F); excursions permitted from 15°C and 30°C (59°F to 86°F).
• Dispense to patient in original container only.
• Store in original container to protect from moisture.
• Replace cap securely each time after opening.
• Do not discard desiccant.

• Dailymed label info on Belumosudil
• FDA Belumosudil

Belumosudil Resources
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