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REZUROCK is a brand name for Belumosudil, supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: REZUROCK is indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (GVHD) after failure of at least two prior lines of systemic therapy. Efficacy in patients with chronic GVHD was based on objective response rate and duration of response in a single-arm…
Verbatim from this product's HC label. Tap a section to expand.
1 Dosing Considerations • Treatment with REZUROCK has not been studied in patients with pre-existing severe renal or hepatic impairment. For patients with pre-existing severe renal or hepatic impairment, consider the risks and potential benefits before initiating treatment with REZUROCK (see 10 CLINICAL PHARMACOLOGY, Special Populations and Conditions).
Product Monograph REZUROCK (Belumosudil tablets) Page 5 of 35 • A complete blood count (CBC), renal function (creatinine) and liver function tests (LFTs) should be performed prior to starting REZUROCK. • Coadministration of rifampin, a strong CYP3A inducer, decreased plasma belumosudil concentrations.
Avoid coadministration of REZUROCK with strong CYP3A inducers. If coadministration cannot be avoided, increase the dose of REZUROCK to 200 mg twice daily (see 9 DRUG INTERACTIONS). • Coadministration of rabeprazole and omeprazole decreased plasma belumosudil concentrations.
Coadministration of REZUROCK with proton pump inhibitors may decrease belumosudil exposure. Increase the dose of REZUROCK to 200 mg twice daily when coadministered with a proton pump inhibitor (see 9 DRUG INTERACTIONS). • Pregnancy testing is recommended for women of childbearing potential prior to initiating REZUROCK.
2 Recommended Dose and Dosage Adjustment The recommended dose of REZUROCK is 200 mg given orally once daily, with food, at approximately the same time each day. Treatment should continue until progression of chronic GVHD that requires a new systemic therapy or occurrence of unacceptable toxicity.
Pediatrics Health Canada has not authorized an indication for pediatric use in patients under the age of 12 years. 1 Pediatrics). Geriatrics No dose adjustment is required in patients ≥ 65 years of age (see 10 CLINICAL PHARMACOLOGY, Special Populations and Conditions).
Recommended Dose Modifications for Adverse Reactions The recommended REZUROCK dosage modifications in case of adverse reactions are provided in Table 1. 5 to 3 x ULN) Hold REZUROCK until recovery to ≤ Grade 1, then resume REZUROCK at the recommended dose.
4 Administration The recommended dose of REZUROCK is 200 mg given orally once daily until progression of chronic GVHD that requires new systemic therapy. Instruct the patient on the following: • Swallow REZUROCK tablets whole. Do not cut, crush, or chew tablets.
5 to 3 x ULN) Hold REZUROCK until recovery to ≤ Grade 1, then resume REZUROCK at the recommended dose. 4 Administration The recommended dose of REZUROCK is 200 mg given orally once daily until progression of chronic GVHD that requires new systemic therapy.
Instruct the patient on the following: • Swallow REZUROCK tablets whole. Do not cut, crush, or chew tablets. 3 Pharmacokinetics). Treatment with REZUROCK has not been studied in patients with pre-existing severe renal or hepatic impairment.
3 Pharmacokinetics). 5 Missed Dose In the event of a missed daily dose of REZUROCK, the missed dose should be taken as soon as possible on the same day. Resume the regular daily dose schedule for REZUROCK the next day. Patients should not take extra doses to make up for the missed dose.
5 OVERDOSAGE There is limited experience with overdose in clinical trials with REZUROCK. There is no known antidote for overdoses with REZUROCK. In the event of suspected overdose, undertake general supportive measures, and observe until clinical stabilization.
For management of a suspected drug overdose, contact your regional poison control centre. Table 1 Recommended Dosage Modifications for REZUROCK for Adverse Reactions Adverse Reaction Severity* REZUROCK Dosage Modifications Grade 4 ALT or AST (> 20 x ULN) or Grade >3 bilirubin (> 3 x ULN) Permanently discontinue REZUROCK.
Other adverse reactions (see 8 ADVERSE REACTIONS) Grade 3 Hold REZUROCK until recovery to ≤ Grade 1, then resume REZUROCK at the recommended dose level. Grade 4 Permanently discontinue REZUROCK. Product Monograph REZUROCK (Belumosudil tablets) Page 7 of 35 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING Table – Dosage Forms, Strengths, Composition and Packaging REZUROCK is available as 200 mg pale yellow, oblong tablets, debossed with “KDM” on one side and “200” on the other side.
1 Special Populations). 2 CONTRAINDICATIONS REZUROCK is contraindicated in patients who are hypersensitive to this drug or to any ingredient in the formulation, including any non-medicinal ingredient, or component of the container. For a complete listing, see 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING.
1 Dosing Considerations • Treatment with REZUROCK has not been studied in patients with pre-existing severe renal or hepatic impairment. For patients with pre-existing severe renal or hepatic impairment, consider the risks and potential benefits before initiating treatment with REZUROCK (see 10 CLINICAL PHARMACOLOGY, Special Populations and Conditions).
Product Monograph REZUROCK (Belumosudil tablets) Page 5 of 35 • A complete blood count (CBC), renal function (creatinine) and liver function tests (LFTs) should be performed prior to starting REZUROCK. • Coadministration of rifampin, a strong CYP3A inducer, decreased plasma belumosudil concentrations.
Avoid coadministration of REZUROCK with strong CYP3A inducers. If coadministration cannot be avoided, increase the dose of REZUROCK to 200 mg twice daily (see 9 DRUG INTERACTIONS). • Coadministration of rabeprazole and omeprazole decreased plasma belumosudil concentrations.
Coadministration of REZUROCK with proton pump inhibitors may decrease belumosudil exposure. Increase the dose of REZUROCK to 200 mg twice daily when coadministered with a proton pump inhibitor (see 9 DRUG INTERACTIONS). • Pregnancy testing is recommended for women of childbearing potential prior to initiating REZUROCK.
2 Recommended Dose and Dosage Adjustment The recommended dose of REZUROCK is 200 mg given orally once daily, with food, at approximately the same time each day. Treatment should continue until progression of chronic GVHD that requires a new systemic therapy or occurrence of unacceptable toxicity.
REZUROCK is contraindicated in patients who are hypersensitive to this drug or to any ingredient in the formulation, including any non-medicinal ingredient, or component of the container. For a complete listing, see 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING.
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3 Pharmacokinetics). Treatment with REZUROCK has not been studied in patients with pre-existing severe renal or hepatic impairment. 3 Pharmacokinetics). 5 Missed Dose In the event of a missed daily dose of REZUROCK, the missed dose should be taken as soon as possible on the same day.
Resume the regular daily dose schedule for REZUROCK the next day. Patients should not take extra doses to make up for the missed dose.
5 mg belumosudil mesylate). REZUROCK is packaged in 60 cc high density polyethylene (HDPE) bottles each containing 30 tablets. 7 WARNINGS AND PRECAUTIONS Cardiovascular Hypertension Of the 83 patients with chronic GVHD who received the recommended dose of 200 mg once daily, hypertension occurred in 21% of patients, including Grade 3-4 hypertension in 6% of patients.
7% of patients had a concomitant medical condition of hypertension. Optimize blood pressure prior to initiating REZUROCK. Consider monitoring blood pressure monthly and/or as clinically indicated. Withhold or permanently discontinue REZUROCK based on severity (see 4 DOSAGE AND ADMINISTRATION).
Hypotension Based on the on-target effect of pan-ROCK inhibitors and the observed lowering of blood pressure in nonclinical studies, hypotension is a potential risk with belumosudil treatment. 2% of subjects experienced at least one TEAE of hypotension or systolic blood pressure < 90 mm Hg respectively.
4% of subjects requiring dose interruption. Optimize blood pressure prior to initiating REZUROCK. Consider monitoring blood pressure monthly and/or as clinically indicated. Withhold or permanently discontinue REZUROCK based on severity (see 4 DOSAGE AND ADMINISTRATION).
Route of Administration Dosage Form / Strength/Composition Non-medicinal Ingredients Oral Tablets 200 mg belumosudil (as belumosudil mesylate) Colloidal silicon dioxide, croscarmellose sodium, hypromellose, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polyvinyl alcohol, talc, titanium dioxide and yellow iron oxide.
5%, with Grade ≥ 3 diarrhea in 5% of patients. A fatal adverse reaction was reported in one patient with severe nausea, vomiting, diarrhea and multi-organ failure; relevant medical history included acute myeloid leukemia, chronic kidney disease, cardiac disorder, and hypertension (see 8 ADVERSE REACTIONS).
To prevent dehydration, administer fluid and electrolyte replacement and antidiarrheal medications as needed. Withhold or permanently discontinue REZUROCK based on severity (see 4 DOSAGE AND ADMINISTRATION). 8%) and anemia (12%) were reported.
4% of patients, 2 patients experienced on-treatment shifts from Grade 0 to Grade 4 (see 8 ADVERSE REACTIONS). Patients should have their complete blood counts monitored monthly. Withhold or permanently discontinue REZUROCK based on severity (see 4 DOSAGE AND ADMINISTRATION).
Hemorrhage Of the 83 patients with chronic GVHD who received the recommended dose of 200 mg once daily, Grade ≥ 3 hemorrhagic events, mainly contusion and hematoma, occurred in 5% of patients treated with REZUROCK. Withhold or permanently discontinue REZUROCK based on severity (see 4 DOSAGE AND ADMINISTRATION).
Hepatic Of the 83 patients with chronic GVHD who received the recommended dose of 200 mg once daily, hepatotoxicity events occurred (see 8 ADVERSE REACTIONS). Liver function test (LFT) elevations, including […]
Pediatrics Health Canada has not authorized an indication for pediatric use in patients under the age of 12 years. 1 Pediatrics). Geriatrics No dose adjustment is required in patients ≥ 65 years of age (see 10 CLINICAL PHARMACOLOGY, Special Populations and Conditions).
Recommended Dose Modifications for Adverse Reactions The recommended REZUROCK dosage modifications in case of adverse reactions are provided in Table 1. Table 1 Recommended Dosage Modifications for REZUROCK for Adverse Reactions Adverse Reaction Severity* REZUROCK Dosage Modifications Hepatotoxicity (see