REZUROCK (belumosudil mesylate)
REZUROCK is indicated for the treatment of Graft-Versus-Host Disease.
How REZUROCK Works
Belumosudil is an inhibitor of rho-associated, coiled-coil containing protein kinases (ROCK), with significantly higher potency for ROCK2 than ROCK1. It modulates immune responses by regulating STAT3/STAT5 phosphorylation, shifting the Th17/Treg cell balance toward an anti-inflammatory state, and inhibiting aberrant pro-fibrotic signaling pathways.
Development Insights
Details
- Status
- Prescription
- First Approved
- 2021-07-16
- Patent Cliff
- 2042
- Revenue
- $125M (Q4-2025)
- Routes
- ORAL
- Dosage Forms
- TABLET
REZUROCK Approval History
What REZUROCK Treats
1 indicationsREZUROCK is approved for 1 conditions since its original approval in 2021. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Graft-Versus-Host Disease
REZUROCK Target & Pathway
ProTarget
REZUROCK Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
Drugs Similar to REZUROCK
FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
23 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT06476132 CLAD | DAIT CTOT-47 | Ph 2 | recruiting | Belumosudil to Block Chronic Lung Allograft Dysfunction (CLAD) in High Risk Lung Transplant Recipients |
| NCT07135973 | LPS18471 | Ph 4 | not yet recruiting | A Study to Investigate Safety of Belumosudil in Participants Aged 12 Years and Above, With Chronic Graft-versus-host Disease (cGVHD) |
| NCT07116031 schoolROCK | DFI17893 U1111-1281-0103, 2024-511508-18 | Ph 2 | recruiting | A Study of Belumosudil in Children With Chronic Graft Versus Host Disease (schoolROCK) |
| NCT06046248 | NSH 1385 | Ph 2 | recruiting | Belumosudil and Rituximab for Primary Treatment of Chronic Graft-Versus-Host-Disease |
| NCT07006506 | 25-033 | Ph 2 | recruiting | A Study of Belumosudil in People at Risk of Developing Graft-Versus-Host Disease After a Stem Cell Transplant |
| NCT06082037 ROCKaspire | EFC17801 U1111-1280-6777, 2023-503462-23 | Ph 3 | recruiting | A Study to Test How Effective Belumosudil Tablets Are for Treating Adult Participants With Chronic Lung Allograft Dysfunction |
| NCT04643002 | ACT16482 U1111-1244-2598, 2024-514988-25 | Ph 1, Ph 2 | recruiting | Isatuximab in Combination With Novel Agents in RRMM - Master Protocol |
| NCT07484113 | IRB-83208 | Ph 1 | not yet recruiting | IL6-receptor Inhibitor Iwith Belumosudil for the Treatment of Belumosudil-refractory cGVHD |
| NCT06105554 | 2023-0527 NCI-2023-09082 | Ph 1, Ph 2 | recruiting | Phase I/II Open Label Study of Belumosudil Mesylate Alone, and in Combination With Dexamethasone, in Patients With Relapsed/Refractory Multiple Myeloma |
| NCT05996627 | RG1123523 NCI-2023-05293, RG1123523 | Ph 2 | recruiting | Belumosudil for the Pre-emptive Treatment of Patients With Chronic Graft Versus Host Disease |
| NCT05567406 | SFY17661 U1111-1277-6715, KD025-218 | Ph 2 | withdrawn | Safety and Efficacy of Oral Belumosudil in Black or African American, American Indian or Alaska Native, and Native Hawaiian or Other Pacific Islander Male and Female Participants Aged 12 Years and Above With Chronic Graft Versus Host Disease (cGVHD) After At Least 2 Prior Lines of Systemic Therapy |
| NCT05922761 | 23-043 | Ph 2 | recruiting | BElumosudil for Bronchiolitis Obliterans Prevention/Therapy (BEBOP) |
| NCT06143891 ROCKnrol-1 | EFC17757 2023-505394-32, U1111-1280-4918 | Ph 3 | active not recruiting | A Study to Test an Oral Medicine, Belumosudil, in Combination With Corticosteroids in Participants at Least 12 Years of Age With Newly Diagnosed Chronic Graft Versus Host Disease. |
| NCT05806567 | INT17676 U1111-1277-6732 | Ph 1 | completed | A Study to Assess the Effect of Oral Belumosudil on Inhibition of Various Proteins in the Fed State in Healthy Male Subjects |
| NCT06616415 | ACT18369 | Ph 4 | active not recruiting | A Clinical Study to Evaluate the Pharmacokinetics, Efficacy, and Safety of Belumosudil in Chinese Adolescents With cGVHD Who Have Had an Inadequate Response to Glucocorticoids or Other Systemic Therapies |
| NCT05918588 | KD025-102 U1111-1290-9646 | Ph 1 | completed | A Study to Determine the Effect of Multiple Oral Doses and Regimens of KD025 in Healthy Male and Post-menopausal Female Subjects |
| NCT05918627 | SLx-2119-09-01 U1111-1291-6021 | Ph 1 | completed | A Study to Determine the Effect of Multiple Oral Doses of SLx-2119 in Healthy Male Subjects |
| NCT05918614 | KD025-103 U1111-1290-9655 | Ph 1 | completed | A Study to Determine the Effect of 500 mg Oral Dose of KD025 in Healthy Male and Post-menopausal Female Subjects |
| NCT04680975 dcSSC results posted | ACT17634 KD025-215 | Ph 2 | terminated | Efficacy and Safety of Belumosudil in Subjects With Diffuse Cutaneous Systemic Sclerosis |
| NCT02688647 results posted | KD025-207 | Ph 2 | completed | A 2-Part, Phase 2 Open-label and Crossover Study of Belumosudil for Treatment of Idiopathic Pulmonary Fibrosis |
| NCT03530995 results posted | KD025-107 2018-000316-16 | Ph 1 | completed | Drug-drug Interaction Between Belumosudil, Itraconazole, Rifampicin, Rabeprazole, and Omeprazole in Healthy Volunteers |
| NCT02106195 results posted | KD025-205 | Ph 2 | completed | A Safety and Tolerability Study of Belumosudil (KD025) Treatment in Subjects With Moderately Severe Psoriasis Vulgaris |
| NCT02852967 results posted | KD025-211 | Ph 2 | completed | A Phase 2, Double-blind, Placebo-controlled Study of the Efficacy and Safety of Belumosudil in Subjects With Moderate/Severe Chronic Plaque Psoriasis |
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
REZUROCK FDA Label Details
Indications & Usage
FDA Label (PDF)REZUROCK is indicated for the treatment of Graft-Versus-Host Disease.
REZUROCK Patents & Exclusivity
Patents (5 active)
Exclusivity
Pro Intelligence Preview
Deep insights for REZUROCK
Revenue Insights
- • Q4-2025: $125M
- • Historical trend analysis
Patent Timeline
- • Cliff: 2042
- • 7 active patents
Trial Analysis
- • 24 total trials
- • Stage: Growth
Competitive Landscape
- • 1 similar drugs
- • Same target/indication analysis
Full approval history • All patents • Revenue trends • Competitor analysis
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.
How We Calculate These Metrics
Trial Activity Stage
Measures the current development activity pattern based on trial phases, status, and trends. Important: This measures R&D activity, not commercial lifecycle.
Trial statuses: "Active" means recruiting or ongoing. "Completed" means reached planned endpoint. "Terminated" means stopped early—often due to safety, efficacy, or business reasons.
- Growth: High proportion of early-phase trials (Phase 1/2), active development
- Expansion: Significant Phase 3 activity, approaching or pursuing approvals
- Mature: Substantial Phase 4 post-marketing studies
- Stable: Mixed phase distribution, steady development
- Declining: Low active trial ratio, reduced R&D investment