belumosudil
Trade name: Rezurock
Small moleculeapprovedOrphan Drug FDABreakthrough Therapy FDA
Approved
Jul 16, 2021
Clinical trial activity
35 trials · 19 clinical orgs · 1 marketing orgs
Phase 1
12
Phase 2
21
Phase 3
2
Phase 4
2
Earliest trial started Sep 21, 2009 (NCT05918627)
Timeline
Indications
Approved for
Studied for
- Autoimmune Diseases · Phase 1
- Biological Availability · Phase 1
- Bronchiolitis · Phase 2
- Bronchiolitis Obliterans · Phase 2
- Colorectal Neoplasms · Early Phase 1
- Drug Interactions · Phase 1
- Fibrosis · Phase 1
- Graft vs Host Disease · Phase 4
- Healthy Volunteers · Phase 1
- Hematologic Neoplasms · Phase 2
- Idiopathic Pulmonary Fibrosis · Phase 2
- Immune Tolerance · Phase 1
- Kidney Diseases · Phase 2
- Kidney Failure, Chronic · Phase 1
- Liver Diseases · Phase 1
- Lung Diseases · Phase 2
- Lung Transplantation · Phase 3
- Multiple Myeloma · Phase 1/Phase 2
- Neoplasms · Early Phase 1
- Psoriasis · Phase 2
- Renal Insufficiency, Chronic · Phase 1
- Scleroderma, Diffuse · Phase 2
- Sclerosis · Phase 2
Mechanism of action
- Rho-associated protein kinase 2ANTAGONIST
ROCK2 antagonist
- Rho-associated protein kinaseINHIBITOR
Rho-associated protein kinase inhibitor
Higher potency against ROCK2 vs. ROCK1
- Rho-associated protein kinase 2INHIBITOR
Rho-associated protein kinase 2 inhibitor
Also active against ROCK1 but higher potency against ROCK2
Approval history
- approvedPriority reviewBreakthroughJul 16, 2021
Chemistry & pharmacology
Loading structure…
SMILES
CC(C)NC(=O)COc1cccc(-c2nc(Nc3ccc4[nH]ncc4c3)c3ccccc3n2)c1- Mol. weight
- 452.52 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
First in class
Sources
- ChEMBLCHEMBL4802130 ↗
- ChEMBLCHEMBL2005186 ↗
Also known as
- kd025
- kd025
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07135973 | Phase 4 | Nov 28, 2025 | Sanofi |
| NCT07116031 | Phase 2 | Oct 31, 2025 | Sanofi |
| NCT07006506 | Phase 2 | May 21, 2025 | Memorial Sloan-Kettering Cancer Center |
| NCT06751602 | Phase 2 | Apr 15, 2025 | The University of Texas, Dallas |
| NCT06616415 | Phase 4 | Nov 7, 2024 | Sanofi |
| NCT06476132 | Phase 2 | Oct 1, 2024 | Duke University, National Institute of Allergy and Infectious Diseases (NIAID) |
| NCT06509490 | N/A | Jul 17, 2024 | Chinese Academy of Medical Sciences |
| NCT06105554 | Phase 1/Phase 2 (Phase 2) | Apr 30, 2024 | Sanofi-Aventis, University of Texas at Houston |
| NCT05922761 | Phase 2 | Dec 31, 2023 | Harvard University, National Heart, Lung, and Blood Institute (NHLBI), Sanofi |
| NCT06046248 | Phase 2 | Dec 31, 2023 | Northside Hospital, Inc., Sanofi |
| NCT05996627 | Phase 2 | Dec 6, 2023 | Sanofi, University of Washington |
| NCT06143891 | Phase 3 | Nov 30, 2023 | Sanofi |
| NCT06082037 | Phase 3 | Oct 10, 2023 | Sanofi |
| NCT05806749 | Phase 1 | Jul 7, 2023 | University of California, Los Angeles |
| NCT05567406 | Phase 2 | Dec 26, 2022 | Kadmon, Sanofi |
| NCT05806567 | Phase 1 | Jul 27, 2022 | Kadmon, Sanofi |
| NCT05382377 | Early Phase 1 (Phase 1) | May 17, 2022 | KAEDI, People's Liberation Army of China |
| NCT05305989 | Phase 2 | Feb 23, 2022 | Kadmon |
| NCT04930562 | Phase 2 | Feb 1, 2021 | BioNova Pharmaceuticals (Shanghai) LTD., Soochow University |
| NCT04680975 | Phase 2 | Jan 20, 2021 | Kadmon |
Showing 20 of 35 trials
Page 1 / 2
Organizations
Research & Development (19)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Kadmon | For profit | 19 | 19 | 2 | 2009 |
| Sanofi | For profit | 13 | 5 | 4 | 2009 |
| Quotient | For profit | 4 | 0 | 1 | 2015 |
| BioNova Pharmaceuticals (Shanghai) LTD. | For profit | 1 | 1 | 1 | 2021 |
| Chinese Academy of Medical Sciences | Academic/Hospital | 1 | 1 | 1 | 2024 |
| Duke University | Academic/Hospital | 1 | 0 | 1 | 2024 |
| Harvard University | Academic/Hospital | 1 | 1 | 1 | 2023 |
| KAEDI | Academic/Hospital | 1 | 0 | 1 | 2022 |
| Memorial Sloan-Kettering Cancer Center | Academic/Hospital | 1 | 1 | 1 | 2025 |
| National Heart, Lung, and Blood Institute (NHLBI) | Government | 1 | 0 | 1 | 2023 |
| National Institute of Allergy and Infectious Diseases (NIAID) | Government | 1 | 1 | 1 | 2024 |
| Northside Hospital, Inc. | Academic/Hospital | 1 | 1 | 1 | 2023 |
| People's Liberation Army of China | Government | 1 | 1 | 1 | 2022 |
| Sanofi-Aventis | For profit | 1 | 0 | 1 | 2024 |
| Soochow University | Academic/Hospital | 1 | 0 | 1 | 2021 |
| The University of Texas, Dallas | Academic/Hospital | 1 | 1 | 1 | 2025 |
| University of California, Los Angeles | Academic/Hospital | 1 | 1 | 1 | 2023 |
| University of Texas at Houston | Academic/Hospital | 1 | 1 | 1 | 2024 |
| University of Washington | Academic/Hospital | 1 | 1 | 1 | 2023 |
19 organizations
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