Version October 2024
Graft-versus-host disease, chronic: Oral: 200 mg once daily until progression of chronic graft-vs-host disease that requires new systemic therapy or until unacceptable toxicity (Ref).
Missed dose: If a dose is missed, do not administer extra doses to make up the missed dose.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
eGFR ≥30 mL/minute/1.73 m2: There are no dosage adjustments provided in the manufacturer's labeling; however, no clinically meaningful differences in belumosudil pharmacokinetics were observed in mild and moderate renal impairment.
eGFR <30 mL/minute/1.73 m2: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); consider risks versus potential benefits of initiating belumosudil in patients with severe renal impairment.
Hepatic impairment at treatment initiation:
Mild impairment (Child-Turcotte-Pugh class A): No dosage adjustment necessary.
Moderate to severe impairment (Child-Turcotte-Pugh class B or C) without liver graft-versus-host disease: Avoid use.
Hepatotoxicity during treatment:
Grade 3 AST or ALT elevation (5 to 20 times ULN) or grade 2 bilirubin elevation (1.5 to 3 times ULN): Hold belumosudil until recovery of bilirubin, AST and ALT to grade 0 or 1, then resume belumosudil at the recommended dose.
Grade 4 AST or ALT elevation (>20 times ULN) or ≥ grade 3 bilirubin elevation (>3 times ULN): Permanently discontinue belumosudil.
Grade 3 adverse reaction: Hold belumosudil until recovery to grade 0 or 1, then resume belumosudil at the recommended dose level.
Grade 4 adverse reaction: Permanently discontinue belumosudil.
Refer to adult dosing.
(For additional information see "Belumosudil: Pediatric drug information")
Graft-versus-host disease, chronic (cGVHD), treatment: Children ≥12 years and Adolescents: Oral: 200 mg once daily until progression of cGVHD that requires new systemic therapy or until unacceptable toxicity (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Dosage adjustment for toxicity:
Children ≥12 years and Adolescents: Oral:
Grade 3 adverse reactions: Withhold belumosudil until recovery to grade 0 to 1, then resume belumosudil at recommended dose level.
Grade 4 adverse reactions: Permanently discontinue belumosudil.
Children ≥12 years and Adolescents: Oral:
Baseline kidney impairment:
GFR ≥30 mL/minute/1.73 m2: There are no dosage adjustments provided in the manufacturer's labeling; however, no clinically meaningful differences in belumosudil pharmacokinetics were observed in mild and moderate kidney impairment.
GFR <30 mL/minute/1.73 m2: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied). Consider the risks versus the potential benefits of belumosudil prior to initiating therapy in patients with severe kidney impairment.
Children ≥12 years and Adolescents: Oral:
Baseline liver impairment:
Mild liver impairment: No dosage adjustment necessary.
Moderate to severe liver impairment without liver graft-versus-host disease: Avoid use.
Hepatotoxicity during treatment:
Grade 3 AST or ALT (5 to 20 times ULN) or grade 2 bilirubin (1.5 to 3 times ULN): Withhold belumosudil until recovery of AST, ALT, and bilirubin to grade 0 to 1, then resume belumosudil at recommended dose.
Grade 4 AST or ALT (>20 times ULN) or ≥ grade 3 bilirubin (>3 times ULN): Permanently discontinue belumosudil.
Infection, including serious infection, has been reported with belumosudil; however, trials involve patients with chronic graft-vs-host disease currently receiving or who previously received known immunosuppressant agents (standard of care) which are associated with an increased risk of infection, thereby making it difficult to ascertain the risk of infection associated with belumosudil (Ref).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Cardiovascular: Edema (27%), hypertension (21%)
Dermatologic: Pruritus (11%), skin rash (12%)
Endocrine & metabolic: Decreased serum calcium (12%), decreased serum phosphate (28%), increased gamma-glutamyl transferase (21%)
Gastrointestinal: Abdominal pain (22%), decreased appetite (17%), diarrhea (35%), dysphagia (16%), nausea (42%)
Hematologic & oncologic: Decreased hemoglobin (11%; grades 3/4: 1%), hemorrhage (23%; grade 3/4: 5%), lymphocytopenia (29%; grades 3/4: 13%)
Infection: Bacterial infection (16%), infection (53%), viral infection (19%)
Nervous system: Headache (21%)
Neuromuscular & skeletal: Arthralgia (15%), asthenia (46%), muscle spasm (17%), musculoskeletal pain (22%)
Respiratory: Cough (30%), dyspnea (33%), nasal congestion (12%)
Miscellaneous: Fever (18%)
1% to 10%:
Endocrine & metabolic: Increased serum potassium (7%)
Hematologic & oncologic: Decreased neutrophils (8%; grades 3/4: 4%), decreased platelet count (10%; grade 3/4: 5%)
Hepatic: Increased serum alanine aminotransferase (7%), increased serum alkaline phosphatase (9%)
Renal: Increased serum creatinine (4%)
There are no contraindications listed in the manufacturer's labeling.
Canadian labeling: Hypersensitivity to belumosudil or any component of the formulation.
There are no warnings listed in the manufacturer's labeling.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Rezurock: 200 mg
No
Tablets (Rezurock Oral)
200 mg (per each): $714.99
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Rezurock: 200 mg
Belumosudil is available through authorized specialty pharmacies and specialty distributors. Information is available at https://rezurockhcp.com/obtaining-rezurock/.
Oral: Administer with a meal at approximately the same time each day. Swallow whole; do not cut, crush, or chew tablets.
Oral: Swallow tablets whole with a glass of water; do not cut, crush, or chew tablets. Administer with a meal at approximately the same time daily.
This medication is not on the NIOSH (2016) list; however, it may meet the criteria for a hazardous drug. Belumosudil may cause teratogenicity and reproductive toxicity.
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).
Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.
Graft-vs-host disease, chronic: Treatment of chronic graft-vs-host disease in adult and pediatric patients ≥12 years of age after failure of at least 2 prior lines of systemic therapy.
Belumosudil may be confused with belimumab, belinostat, budesonide.
Substrate of CYP2C8 (minor), CYP2D6 (minor), CYP3A4 (major), P-glycoprotein/ABCB1 (minor), UGT1A9; Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits BCRP/ABCG2, OATP1B1/1B3 (SLCO1B1/1B3), P-glycoprotein/ABCB1
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Afatinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Afatinib. Management: If combined, administer the P-gp inhibitor simultaneously with, or after, the dose of afatinib. Monitor closely for signs and symptoms of afatinib toxicity and if the combination is not tolerated, reduce the afatinib dose by 10 mg. Risk D: Consider therapy modification
Aliskiren: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Aliskiren. Risk C: Monitor therapy
Alpelisib: BCRP/ABCG2 Inhibitors may increase the serum concentration of Alpelisib. Management: Avoid coadministration of BCRP/ABCG2 inhibitors and alpelisib due to the potential for increased alpelisib concentrations and toxicities. If coadministration cannot be avoided, closely monitor for increased alpelisib adverse reactions. Risk D: Consider therapy modification
Antacids: May decrease the serum concentration of Belumosudil. Management: Consider separating administration of belumosudil and antacids by 2 hours and monitor for reduced belumosudil efficacy. Risk D: Consider therapy modification
Atogepant: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Atogepant. Management: For episodic migraine, the recommended atogepant dose is 10 mg or 30 mg once daily if given with OATP1B1/1B3 inhibitors. For chronic migraine, the recommended atogepant dose is 30 mg once daily with OATP1B1/1B3 inhibitors. Risk D: Consider therapy modification
BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors): Belumosudil may increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Management: Avoid coadministration of belumosudil with these substrates of BCRP for which minimal concentration increases can cause serious adverse effects. If coadministration is required, dose reductions of the BCRP substrate may be required. Risk D: Consider therapy modification
Berotralstat: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Berotralstat. Management: Decrease the berotralstat dose to 110 mg daily when combined with P-glycoprotein (P-gp) inhibitors. Risk D: Consider therapy modification
Berotralstat: BCRP/ABCG2 Inhibitors may increase the serum concentration of Berotralstat. Management: Decrease the berotralstat dose to 110 mg daily when combined with BCRP inhibitors. Risk D: Consider therapy modification
Bilastine: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Bilastine. Risk X: Avoid combination
Brincidofovir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Brincidofovir. Management: Consider alternatives to OATP1B/1B3 inhibitors in patients treated with brincidofovir. If coadministration is required, administer OATP1B1/1B3 inhibitors at least 3 hours after brincidofovir and increase monitoring for brincidofovir adverse reactions. Risk D: Consider therapy modification
Celiprolol: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Celiprolol. Risk C: Monitor therapy
Cladribine: BCRP/ABCG2 Inhibitors may increase the serum concentration of Cladribine. Management: Avoid concomitant use of BCRP inhibitors during the 4 to 5 day oral cladribine treatment cycles whenever possible. If combined, consider dose reduction of the BCRP inhibitor and separation in the timing of administration. Risk D: Consider therapy modification
Colchicine: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Colchicine. Colchicine distribution into certain tissues (e.g., brain) may also be increased. Management: This combination is often contraindicated, but combined use may be permitted with dose adjustment and monitoring. Recommendations vary based on brand, indication, use of CYP3A4 inhibitors, and hepatic/renal function. See interaction monograph for details. Risk D: Consider therapy modification
CycloSPORINE (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of CycloSPORINE (Systemic). Risk C: Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of Belumosudil. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of Belumosudil. Management: Increase the dose of belumosudil to 200 mg twice daily when coadministered with strong CYP3A4 inducers. Risk D: Consider therapy modification
Dabigatran Etexilate: P-glycoprotein/ABCB1 Inhibitors may increase serum concentrations of the active metabolite(s) of Dabigatran Etexilate. Risk C: Monitor therapy
Digoxin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Digoxin. Management: Measure digoxin serum concentrations before initiating treatment with these P-glycoprotein (P-gp) inhibitors. Reduce digoxin concentrations by either reducing the digoxin dose by 15% to 30% or by modifying the dosing frequency. Risk D: Consider therapy modification
DOXOrubicin (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of DOXOrubicin (Conventional). Risk X: Avoid combination
DOXOrubicin (Liposomal): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of DOXOrubicin (Liposomal). Risk C: Monitor therapy
Edoxaban: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Edoxaban. Risk C: Monitor therapy
Elagolix: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix. Risk X: Avoid combination
Elagolix, Estradiol, and Norethindrone: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix, Estradiol, and Norethindrone. Specifically, concentrations of elagolix may be increased. Risk X: Avoid combination
Elbasvir and Grazoprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elbasvir and Grazoprevir. Risk X: Avoid combination
Eluxadoline: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Eluxadoline. Management: Decrease the eluxadoline dose to 75 mg twice daily if combined with OATP1B1/1B3 inhibitors and monitor patients for increased eluxadoline effects/toxicities. Risk D: Consider therapy modification
Etoposide: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Etoposide. Risk C: Monitor therapy
Etoposide Phosphate: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Etoposide Phosphate. Risk C: Monitor therapy
Everolimus: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Everolimus. Risk C: Monitor therapy
Histamine H2 Receptor Antagonists: May decrease the serum concentration of Belumosudil. Risk C: Monitor therapy
Inhibitors of the Proton Pump (PPIs and PCABs): May decrease the serum concentration of Belumosudil. Management: Increase the dose of belumosudil to 200 mg twice daily when coadministered with inhibitors of the proton pump (PPIs and PCABs). Risk D: Consider therapy modification
Lapatinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Lapatinib. Risk C: Monitor therapy
Larotrectinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Larotrectinib. Risk C: Monitor therapy
Lefamulin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Lefamulin. Management: Avoid concomitant use of lefamulin tablets with P-glycoprotein/ABCB1 inhibitors. If concomitant use is required, monitor for lefamulin adverse effects. Risk D: Consider therapy modification
Mavorixafor: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Mavorixafor. Risk C: Monitor therapy
Nadolol: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Nadolol. Risk C: Monitor therapy
Naldemedine: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Naldemedine. Risk C: Monitor therapy
Naloxegol: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Naloxegol. Risk C: Monitor therapy
OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors): Belumosudil may increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Management: Avoid coadministration of belumosudil with these substrates of OATP1B1/1B3 for which minimal concentration increases can cause serious adverse effects. If coadministration is required, dose reductions of the OATP1B1/1B3 substrate may be required. Risk D: Consider therapy modification
PAZOPanib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of PAZOPanib. Risk X: Avoid combination
PAZOPanib: BCRP/ABCG2 Inhibitors may increase the serum concentration of PAZOPanib. Risk X: Avoid combination
Pralsetinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Pralsetinib. Management: If this combo cannot be avoided, decrease pralsetinib dose from 400 mg daily to 300 mg daily; from 300 mg daily to 200 mg daily; and from 200 mg daily to 100 mg daily. Risk D: Consider therapy modification
Ranolazine: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Ranolazine. Risk C: Monitor therapy
Relugolix: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Relugolix. Management: Avoid coadministration of relugolix with oral P-gp inhibitors whenever possible. If combined, take relugolix at least 6 hours prior to the P-gp inhibitor and monitor patients more frequently for adverse reactions. Risk D: Consider therapy modification
Relugolix, Estradiol, and Norethindrone: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Relugolix, Estradiol, and Norethindrone. Management: Avoid use of relugolix/estradiol/norethindrone with P-glycoprotein (P-gp) inhibitors. If concomitant use is unavoidable, relugolix/estradiol/norethindrone should be administered at least 6 hours before the P-gp inhibitor. Risk D: Consider therapy modification
Repotrectinib: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Repotrectinib. Risk X: Avoid combination
Resmetirom: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Resmetirom. Risk X: Avoid combination
Revefenacin: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentrations of the active metabolite(s) of Revefenacin. Risk X: Avoid combination
RifAXIMin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of RifAXIMin. Risk C: Monitor therapy
Rimegepant: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Rimegepant. Management: Avoid administration of another dose of rimegepant within 48 hours if given concomitantly with a P-glycoprotein (P-gp) inhibitor. Risk D: Consider therapy modification
RisperiDONE: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of RisperiDONE. Risk C: Monitor therapy
RomiDEPsin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of RomiDEPsin. Risk C: Monitor therapy
Saquinavir: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Saquinavir. Risk C: Monitor therapy
Silodosin: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Silodosin. Risk C: Monitor therapy
Sirolimus (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Sirolimus (Conventional). Management: Avoid concurrent use of sirolimus with P-glycoprotein (P-gp) inhibitors when possible and alternative agents with lesser interaction potential with sirolimus should be considered. Monitor for increased sirolimus concentrations/toxicity if combined. Risk D: Consider therapy modification
Sirolimus (Protein Bound): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Sirolimus (Protein Bound). Risk X: Avoid combination
Tacrolimus (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Tacrolimus (Systemic). Risk C: Monitor therapy
Taurursodiol: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Taurursodiol. Risk X: Avoid combination
Tegaserod (Withdrawn from US Market): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Tegaserod (Withdrawn from US Market). Risk C: Monitor therapy
Teniposide: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Teniposide. Risk C: Monitor therapy
Topotecan: BCRP/ABCG2 Inhibitors may increase the serum concentration of Topotecan. Risk X: Avoid combination
Topotecan: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Topotecan. Risk X: Avoid combination
Ubrogepant: BCRP/ABCG2 Inhibitors may increase the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with a BCRP inhibitor. Risk D: Consider therapy modification
Ubrogepant: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with a P-gp inhibitor. Risk D: Consider therapy modification
UGT1A1 Substrates: Belumosudil may increase the serum concentration of UGT1A1 Substrates. Management: Avoid coadministration of belumosudil with substrates of UGT1A1 for which minimal concentration increases can cause serious adverse effects. If coadministration is required, dose reductions of the UGT1A1 substrate may be required. Risk D: Consider therapy modification
Venetoclax: P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of Venetoclax. Management: Reduce the venetoclax dose by at least 50% in patients requiring concomitant treatment with P-glycoprotein (P-gp) inhibitors. Resume the previous venetoclax dose 2 to 3 days after discontinuation of a P-gp inhibitor. Risk D: Consider therapy modification
VinCRIStine (Liposomal): P-glycoprotein/ABCB1 Inhibitors may increase the serum concentration of VinCRIStine (Liposomal). Risk X: Avoid combination
Voxilaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Voxilaprevir. Risk X: Avoid combination
Zavegepant: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Zavegepant. Risk X: Avoid combination
Belumosudil Cmax and AUC increased 2.2 times and 2 times, respectively, following administration of a single belumosudil dose with a high-fat and high-calorie meal (800 to 1,000 calories with ~50% of calories from fat) compared to the fasted state (in healthy subjects). Management: Administer with a meal.
Verify pregnancy status prior to use in patients who may become pregnant.
Patients who may become pregnant and patients with partners who may become pregnant should use effective contraception during therapy and for 1 week after the last belumosudil dose.
Based on data from animal studies, belumosudil may reversibly impair fertility.
Based on the mechanism of action and data from animal reproduction studies, in utero exposure to belumosudil may cause fetal harm.
It is not known if belumosudil is present in breast milk.
Due to the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer during therapy and for 1 week after the last belumosudil dose.
Monitor total bilirubin, AST, and ALT at least monthly. Verify pregnancy status prior to use in patients who may become pregnant. Monitor adherence.
Belumosudil is a kinase inhibitor which selectively inhibits rho-associated, coiled-coil containing protein kinase (ROCK), predominantly inhibiting ROCK2 and to a lesser extent, ROCK1. ROCK2 inhibition downregulates signal transducer and activator of transcription 3 (STAT3) phosphorylation and decreases expression of type 17 helper T-cell (Th17) transcription factors (Cutler 2021). ROCK2 inhibition also restores immune system balance via upregulation of signal transducer and activator of transcription 5 (STAT5), which results in shifting Th17/regulatory T-cell balance (Jagasia 2021). Belumosudil inhibition of ROCK2 results in downregulation of proinflammatory responses and inhibits aberrant profibrotic signaling.
Distribution: Vd: 184 L.
Protein binding: 99.9% (to human serum albumin); 98.6% to human alpha 1-acid glycoprotein.
Metabolism: Primarily by CYP3A4 and to a lesser extent by CYP2C8, CYP2D6, and UGT1A9.
Bioavailability: 64%.
Half-life elimination: 19 hours.
Time to peak: ~1.3 to 2.5 hours (delayed ~0.5 hours with a high-fat/high-calorie meal).
Excretion: Feces: 85% (30% as unchanged drug); urine: <5%.
Clearance: 9.83 L/hour.
Hepatic function impairment: Total concentrations of AUC increased 1.4-fold, 1.5-fold, and 4.2-fold, respectively, in patients with mild, moderate, or severe impairment compared to patients with normal hepatic function. AUC of free concentrations decreased 19%, increased 1.4-fold, and increased 16-fold, respectively, in patients with mild, moderate, or severe impairment compared to patients with normal hepatic function.
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