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Rezurock (BELUMOSUDIL)
Rezurock works by inhibiting the Rho-associated protein kinase 1 enzyme, which plays a key role in inflammation and immune response.
At a glance
| Generic name | BELUMOSUDIL |
|---|---|
| Sponsor | Kadmon Pharms Llc |
| Target | Rho-associated protein kinase 1 |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
| First approval | 2021 |
Mechanism of action
Belumosudil is an inhibitor of rho-associated, coiled-coil containing protein kinase (ROCK) which inhibits ROCK2 and ROCK1 with IC 50values of approximately 100 nM and uM, respectively. Belumosudil down-regulated proinflammatory responses via regulation of STAT3/STAT5 phosphorylation and shifting Th17/Treg balance in ex-vivo or in vitro-human cell assays. Belumosudil also inhibited aberrant pro-fibrotic signaling, in vitro. In vivo, belumosudil demonstrated activity in animal models of chronic GVHD.
Approved indications
- Chronic graft-versus-host disease (chronic GVHD)
Common side effects
- Infections
- Asthenia
- Nausea
- Diarrhea
- Dyspnea
- Cough
- Edema
- Hemorrhage
- Abdominal pain
- Musculoskeletal pain
- Headache
- Phosphate decreased
Key clinical trials
- A Study to Test How Effective Belumosudil Tablets Are for Treating Adult Participants With Chronic Lung Allograft Dysfunction (PHASE3)
- A Study of Belumosudil in People at Risk of Developing Graft-Versus-Host Disease After a Stem Cell Transplant (PHASE2)
- IL6-receptor Inhibitor Iwith Belumosudil for the Treatment of Belumosudil-refractory cGVHD (PHASE1)
- A Study to Investigate Safety of Belumosudil in Participants Aged 12 Years and Above, With Chronic Graft-versus-host Disease (cGVHD) (PHASE4)
- A Study of Belumosudil in Children With Chronic Graft Versus Host Disease (schoolROCK) (PHASE2)
- Evaluation of Belumosudil Whole Tablets vs. Crushed Tablets Pharmacokinetics in Patients Suffering From Chronic GvHD
- Phase I/II Open Label Study of Belumosudil Mesylate Alone, and in Combination With Dexamethasone, in Patients With Relapsed/Refractory Multiple Myeloma (PHASE1,PHASE2)
- Belumosudil for the Pre-emptive Treatment of Patients With Chronic Graft Versus Host Disease (PHASE2)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |