Nurses Compass
Drug Guide
Belumosudil Mesylate
Classification
Therapeutic: Immunosuppressant
Pharmacological: ROCK2 inhibitor
FDA Approved Indications
- Prophylaxis of graft-versus-host disease (GVHD) in adult and pediatric patients 12 years and older.
Mechanism of Action
Belumosudil inhibits Rho-associated coiled-coil containing protein kinase 2 (ROCK2), leading to modulation of immune responses and reduction of inflammatory pathways involved in GVHD.
Dosage and Administration
Adult: Starting dose of 200 mg once daily, adjustable based on response and tolerability.
Pediatric: Dose adjustments based on weight and therapeutic response; consult specific pediatric dosing guidelines.
Geriatric: No specific dose adjustment required, but tol erance should be monitored carefully.
Renal Impairment: No specific adjustment recommended; however, renal function should be monitored regularly.
Hepatic Impairment: No specific adjustment recommended.
Pharmacokinetics
Absorption: Orally administered; peak plasma concentration typically reached within 4-6 hours.
Distribution: High protein binding (~98%), primarily to albumin.
Metabolism: Primarily metabolized by CYP3A4 enzyme; minor pathways include CYP2C19.
Excretion: Metabolites are excreted mainly in feces; minor urinary excretion.
Half Life: Approximately 4 days (96 hours).
Contraindications
- Hypersensitivity to belumosudil or any component of the formulation.
Precautions
- Use with caution in patients with hepatic impairment.
- Potential for increased bleeding risk; monitor for signs of bleeding.
- Increased susceptibility to infections; monitor closely.
- Pregnancy Category: C; use only if clearly needed.
Adverse Reactions - Common
- Nausea (Common)
- Diarrhea (Common)
- Fatigue (Common)
- Elevation of liver enzymes (Common)
Adverse Reactions - Serious
- Infections (e.g., pneumonia, herpes zoster) (Serious)
- Hepatotoxicity (Serious)
- Bleeding events (Serious)
Drug-Drug Interactions
- CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase belumosudil levels.
- CYP3A4 inducers (e.g., rifampin) may decrease levels.
Drug-Food Interactions
- No specific food interactions identified.
Drug-Herb Interactions
- St. John's Wort may reduce efficacy by inducing CYP3A4.
Nursing Implications
Assessment: Monitor liver function tests, complete blood counts, and signs of infection or bleeding.
Diagnoses:
- Risk for bleeding related to potential thrombocytopenia.
- Impaired immunity related to immunosuppressive therapy.
Implementation: Administer orally once daily; monitor response and tolerance; educate patient on signs of infection and bleeding.
Evaluation: Assess for reduction in GVHD symptoms and monitor for adverse effects.
Patient/Family Teaching
- Take the medication exactly as prescribed, at the same time each day.
- Report signs of infection, unusual bleeding, or bruising promptly.
- Avoid grapefruit and grapefruit juice, which may increase drug levels.
- Attend regular follow-up appointments for lab tests and assessment.
Special Considerations
Black Box Warnings:
- Serious infections and subsequent complications including death.
- Hepatotoxicity.
Genetic Factors: None specifically identified.
Lab Test Interference: Elevations in liver function tests; may require dose adjustments.
Overdose Management
Signs/Symptoms: Potential toxicity includes severe hepatotoxicity, bleeding, or infections.
Treatment: Supportive care, discontinue drug, and monitor vital signs and laboratory parameters; no specific antidote.
Storage and Handling
Storage: Store at room temperature away from moisture and light.
Stability: Stable for the duration of the shelf life indicated on the label.