Belumosudil

Belumosudil is a prescription medication indicated for chronic graft versus host disease (GVHD) in adults and adolescents aged 12 years and older after the failure of at least 2 prior lines of systemic therapy.

• Belumosudil is available under the following different brand names: Rezurock

Common side effects of Belumosudil include:

• infections
• weakness
• nausea
• diarrhea
• shortness of breath
• cough
• fluid retention (edema)
• bleeding
• abdominal pain
• musculoskeletal pain
• headache
• decreased phosphate
• increased gamma-glutamyl transferase
• decreased lymphocytes
• high blood pressure (hypertension)

Serious side effects of Belumosudil include:

• severe ongoing nausea, vomiting, or diarrhea
• liver problems, including symptoms such as loss of appetite, stomach pain (upper right side), dark urine, jaundice (yellowing of the skin or eyes)
• signs of infection, such as fever, chills, sore throat, body aches, unusual tiredness, bruising or bleeding, painful urination, cough with mucus, chest pain, shortness of breath

Rare side effects of Belumosudil include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Tablet

• 200 mg

Graft-versus-host disease (GVHD)

Adult dosage

• 200 mg orally once a day
• Continue until the progression of chronic GVHD requires new systemic therapy

Pediatric dosage

• Children younger than 12 years: Safety and efficacy not established
• Children aged 12 years and older: 200 mg orally once a day

Dosage Considerations – Should be Given as Follows:

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Belumosudil has severe interactions with no other drugs.
• Belumosudil has serious interactions with the following drug:
  • fexinidazole
• Belumosudil has moderate interactions with at least 43 other drugs.
• Belumosudil has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• None

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Belumosudil?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Belumosudil?”

Cautions

• Can cause fetal harm
• Drug interaction overview
  • Substrate of CYP3A4 and P-glycoprotein (P-gp)
• In vitro studies
  • Inhibits BCRP, P-gp, and OATP1B1 at clinically relevant concentrations
  • Inhibits CYP1A2, CYP2C19, CYP2D6, UGT1A1, and UGT1A9
• Strong CYP3A4 inducers
  • Increase the dose of belumosudil to 200 mg orally two times a day when coadministered with strong CYP3A inducers
• Strong CYP3A inducers decrease exposure and effects of belumosudil
• Proton pump inhibitors
  • Increase the dose of belumosudil to 200 mg orally two times a day when coadministered with proton pump inhibitors
  • Proton pump inhibitors decrease exposure and effects of belumosudil

Pregnancy and Lactation

• Based on animal studies and the drug’s mechanism of action, fetal harm may occur
• No human data are available on the drug’s use in pregnant women to evaluate for any drug-associated risks
• Verify the pregnancy status of women of reproductive potential before initiating belumosudil
• Contraception
  • Women of reproductive potential
  • Use effective contraception during treatment and for at least 1 week after the last dose
  • If used during pregnancy or if the patient becomes pregnant during treatment, inform the patient of the potential hazard to the fetus
  • Male with female partners of reproductive potential
  • Use effective contraception during treatment and for at least 1 week after the last dose
• Infertility
  • Based on animal findings, male or female fertility may be impaired; effects on fertility are reversible
• Lactation
  • There are no data available on the presence of the drug or its metabolites in human milk or its effects on breastfed children and milk production
  • Advise lactating women not to breastfeed during treatment and for at least 1 week after the last dose