Delving into the Latest Updates on Belumosudil Mesilate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Belumosudil Mesylate, 甲磺酸贝舒地尔, BN-101

+ [11]

Target

ROCK1 x ROCK2

Action

inhibitors

Mechanism

ROCK1 inhibitors(Rho-associated protein kinase 1 inhibitors), ROCK2 inhibitors(Rho-associated protein kinase 2 inhibitors)

Therapeutic Areas

Immune System DiseasesOther DiseasesInfectious Diseases+ [3]

Active Indication

Chronic graft-versus-host diseaseAllograft RejectionLung transplant rejection+ [3]

Inactive Indication

Autoimmune DiseasesChronic large plaque psoriasisFibrosis+ [3]

Originator Organization

Kadmon Pharmaceuticals LLC

Active Organization

SanofiKadmon Pharmaceuticals LLC

National Heart, Lung & Blood Institute

+ [7]

Inactive Organization

Bk Pharmaceuticals Ltd

Kadmon Corp. LLCKadmon Holdings, Inc.

License Organization

Surface Logix LLC

Nano Terra, Inc.

BioNova Pharmaceuticals (Shanghai) Ltd.

+ [4]

Drug Highest PhaseApproved

First Approval Date

United States (16 Jul 2021),

Chronic graft-versus-host disease

RegulationBreakthrough Therapy (United States), Orphan Drug (United States), Breakthrough Therapy (China), Orphan Drug (South Korea), Orphan Drug (Australia), Priority Review (Australia), Priority Review (United States)

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Structure/Sequence

Molecular FormulaC27H28N6O5S

InChIKeyILQJXEIRBCHLOM-UHFFFAOYSA-N

CAS Registry2109704-99-4

A Phase 2, Open-label, Multicenter Study to Evaluate the Safety and Efficacy of Belumosudil in Black or African American, American Indian or Alaska Native, and Native Hawaiian or Other Pacific Islander Participants With Chronic Graft Versus Host Disease (cGVHD) After At Least 2 Prior Lines of Systemic Therapy

The purpose of this study is to measure 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 with cGVHD who have previously been treated with at least 2 prior lines of systemic therapy aged 12 years and above.
The duration of participants participation will be up to 4 weeks for screening, treatment until clinically significant progression of disease, and 4 weeks of safety follow-up, and then long-term follow-up every 12 weeks.1 Cycle = 28 days.

Start Date16 Jun 2025

Sponsor / Collaborator

Kadmon Holdings, Inc.

NCT06751602

/ Not yet recruitingPhase 2IIT

A Phase 2, Randomized, Placebo-Controlled Study to Evaluate Belumosudil for the Abrogation of Interstitial Fibrosis and Tubular Atrophy in De Novo Kidney Transplant Recipients

This is a randomized, double-blind, placebo-controlled trial in de novo kidney transplant patients to determine if the addition of belumosudil (brand name- REZUROCK®) on the background of standard immunosuppression will prevent fibrosis in the kidney transplant. Interstitial expansion is the precursor of interstitial fibrosis and graft loss. The hypothesis underlying the study is that abgrogating the fibrogenic effects of the RhoA pathway with belumosudil will reduce structural damage in transplanted kidneys and possible subsequent transplant failure.

Start Date15 Apr 2025

Sponsor / Collaborator

The Methodist Hospital Research Institute

NCT06476132

/ RecruitingPhase 2IIT

Belumosudil to Block Chronic Lung Allograft Dysfunction (CLAD) in High Risk Lung Transplant Recipients: A Randomized, Multicenter, Double Blind, Placebo-Controlled Trial (CTOT-47)

The purpose of this study is to see if taking the study drug, Belumosudil, for 52 weeks in addition to your usual care and medication, will prevent Chronic Lung Allograft Dysfunction (CLAD) in participants who have a lung biopsy that shows evidence of rejection or inflammation to the transplanted lung(s). For this study, biopsies that show evidence of Acute Rejection (AR), Lymphocytic Bronchiolitis (LB), Organizing Pneumonia (OP) or Acute Lung Injury (ALI) are referred to as "Qualifying Biopsies"; patients who had evidence of one or more of these conditions on a recent biopsy are eligible for enrollment in this study. Belumosudil is an investigational drug that blocks a molecule in the body that reduces inflammation and scarring and may play a role in the development and progression of CLAD. Belumosudil is a drug approved by the FDA to treat adults and children 12 years and older with chronic graft-versus-host disease (cGVHD), a condition with some similarities to CLAD.
The primary objective it to determine the efficacy of treatment with Belumosudil + maintenance immunosuppression (IS) versus placebo + maintenance IS on preventing the subsequent development of probable or definite CLAD, lung retransplant, or death.

Start Date12 Mar 2025

Sponsor / Collaborator

National Institute of Allergy & Infectious Diseases

100 Clinical Results associated with Belumosudil Mesilate

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100 Translational Medicine associated with Belumosudil Mesilate

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100 Patents (Medical) associated with Belumosudil Mesilate

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163

Literatures (Medical) associated with Belumosudil Mesilate

01 Jul 2025·BIOCHEMICAL PHARMACOLOGY

The dual targeting effects of KD025 on casein kinase 2 and ROCK2 in a mouse model of diet-induced obesity

Article

Author: Tran, Nhu Nguyen Quynh ; Kim, Min Kyung ; Maeng, Han-Joo ; Oh, Byung-Chul ; Oh, Yu Jin ; Lee, Jeongmi ; Kim, Young-Bum ; Jun, Hee-Sook ; Choi, Hojung ; Sactivel, Bathiga ; Lee, Dae Ho ; Chun, Kwang-Hoon

KD025(belumosudil), a selective ROCK2 inhibitor, exhibits unique anti-adipogenic activity through inhibition of casein kinase 2 (CK2). This study investigated the dual inhibitory effects of KD025 on metabolism in a diet-induced obese model. C57BL/6 mice on a high fat diet (HFD) were treated with KD025 for 4 weeks, while fasudil (a pan-ROCK inhibitor) and CX-4945 (a CK2-specific inhibitor) served as comparison treatments. KD025 significantly reduced body weight gain without affecting food intake, serum insulin, or fasting blood glucose levels. In contrast, while both CX-4945 and fasudil treatments showed a trend toward weight reduction, these results were not statistically significant. KD025 improved lipid metabolism by significantly lowering LDL cholesterol and triglyceride, although it slightly impaired glucose metabolism, as observed in insulin and glucose tolerance tests. Weight reduction in the KD025- and CX-4945-treated groups was attributed to decreased adipose tissue mass, particularly in inguinal (ingWAT) and epididymal (epiWAT) fat depots. Hematoxylin and eosin (H&E) staining confirmed smaller adipocyte size in these groups. KD025 had no significant effect on serum levels of tumor necrosis factor-α (TNF-α), interleukin 6 (IL-6), or monocyte chemoattractant protein-1 (MCP-1) with varied inflammatory responses. Furthermore, KD025 and CX-4945 upregulated adipogenic and browning markers, such as Cebpa, Cidea, and Pparg in the epiWAT, though without significant UCP1 expression. Overall, KD025 effectively reduced weight gain in HFD-fed mice through dual inhibition of CK2 and ROCK2, highlighting its potential as a therapeutic agent for obesity-related conditions.

01 May 2025·Transplantation and Cellular Therapy

Belumosudil for Chronic Graft-Versus-Host Disease: Analysis of Long-Term Results from the KD025-208 and ROCKstar Studies

Article

Author: Lee, Stephanie J ; Cutler, Corey ; Blazar, Bruce R ; Yao, Yu ; Pavletic, Steven ; Marshall, Kathy ; Ji, Ran

Belumosudil is an oral selective rho-associated coiled-coil-containing protein kinase-2 (ROCK2) inhibitor approved for the treatment of chronic graft-versus-host disease (cGVHD) following an allogeneic hematopoietic cell transplant in patients aged ≥12 years after failure of ≥2 prior systemic lines of therapy. The KD025-208 (NCT02841995) and KD025-213 (ROCKstar; NCT03640481) studies demonstrated that belumosudil was well tolerated, with clinically meaningful responses in patients with cGVHD. KD025-217 (NCT05305989) is a follow-up study that evaluated extended treatment with belumosudil in patients enrolled in the parent studies, KD025-208 and ROCKstar. This pooled analysis reports the long-term follow-up (overall median follow-up duration of 31.4 months) results from these studies in patients with cGVHD. The study included a total of 208 patients across 3 cohorts. Cohort 1 (n = 95) received belumosudil 200 mg once daily, cohort 2 (n = 92) received belumosudil 200 mg twice daily, and cohort 3 (n = 21) received belumosudil 400 mg once daily. The primary endpoint was best overall response rate (ORR). Duration of response (DOR), failure-free survival (FFS), and time to next treatment (TTNT) were also evaluated in this analysis. The best ORR in the modified intent-to-treat (mITT) population was 72%. The median DOR for the responder population was 62.3 weeks (range, 36.1 to 82.6 weeks). The median FFS in the mITT population was 15.1 months (range, 11.3 to 20.6 months). The 1- and 2-year FFS rates were 56% and 40%, respectively. The median TTNT was 22.1 months (range, 15.2 to 40.3 months), where 47% of patients received a new systemic therapy for cGVHD by 36 months. When compared with the published data, the long-term results from this pooled analysis of these two phase 2 studies demonstrated belumosudil was associated with durable responses, and it remained well tolerated with no new safety concerns.

13 Apr 2025·Immunotherapy

Evaluating Axatilimab as a treatment option for chronic graft-versus-host disease

Review

Author: Anthias, Chloe ; Dexter, Tania ; Nicholson, Emma

Allogeneic stem cell transplantation represents the only curative option for many patients with high risk hematological malignancies but is associated with a number of severe complications. Of these, chronic graft versus host disease (cGVHD) is the leading cause of late non-relapse mortality and of much morbidity. For over 30 years, glucocorticoids have been the mainstay of first line therapy, yet approximately 50% patients are refractory or dependent and traditionally there have been few options for these patients. In recent years, newer treatments including ruxolitinib and belumosudil have shown success in the second and third line settings. However, further effective nontoxic treatments are a necessary to address this complex debilitating disease. Axatilimab is an antibody to colony stimulating factor 1 (CSF-1), a tyrosine kinase receptor. CSF1R signaling dependent macrophages and monocytes are key mediators of inflammation and fibrosis in chronic GVHD, and thus, this therapy offers a targeted approach. Here we summarize the key clinical studies that have been performed to date of this novel therapy.

54

News (Medical) associated with Belumosudil Mesilate

10 Feb 2025

·pharma.economictimes.indiatimes.com

Sanofi Healthcare gets marketing authorisation for cGVHD drug

New Delhi: Sanofi Healthcare India on Monday said it has received marketing authorisation for a drug used for the treatment of Chronic graft versus host disease (cGVHD). The company has received approval for Rezurock ( Belumosudil tablets ), which represents a new treatment paradigm for cGVHD patients globally (12 years and above) after failure of two previous lines of treatment, including those with difficult-to-treat manifestations like fibrosis . Rezurock was approved by the US Food and Drug Administration ( USFDA ) and by the CDSCO in India in 2024. "This milestone reflects our dedication to addressing unmet medical needs in the transplant ecosystem and delivering breakthrough therapies for patients with this severe condition," Sanofi India MD Rodolfo Hrosz said in a statement. cGVHD is a complication that can occur following allogeneic stem cell transplantation, resulting in significant morbidity and mortality.

Drug ApprovalCell Therapy

25 Dec 2024

·www.pharmaindustrial-india.com

Meiji Seika Pharma Establishes Local Subsidiary Taiwan Meiji Pharma

Meiji Seika Pharma has announced the establishment of a local subsidiary, Taiwan Meiji Pharma Co., Ltd. This subsidiary will focus on pharmaceutical sales and other related activities in Taiwan and is scheduled to commence operations in February 2025. Meiji Seika Pharma aims to become ‘a company in Asia in the field of infectious diseases’ as part of the ‘Meiji Group 2026 Vision’ targeting the year 2026. By establishing Taiwan Meiji Pharma Co., Ltd. in Taiwan, the fifth largest pharmaceutical market in Asia, we aim to build a business foundation and achieve further growth by supplying products. Taiwan Meiji Pharma Co., Ltd. plans to launch ‘REZUROCK’ (product name in Japan, generic name: belumosudil mesylate), a selective ROCK2 inhibitor for the treatment of chronic graft-versus-host disease (Chronic GVHD), which is currently under application for regulatory approval with the Taiwan Food and Drug Administration (TFDA). Chronic GVHD is a disease that occurs following hematopoietic stem cell transplantation performed for the treatment of leukemia.

Drug Approval

25 Dec 2024

·www.businesswire.com

Meiji Seika Pharma: Announcement of the Establishment of Local Subsidiary "Taiwan Meiji Pharma Co., Ltd." in Taiwan

TOKYO--( BUSINESS WIRE )--Meiji Seika Pharma Co., Ltd. (Headquarters: Chuo-ku, Tokyo, President: Daikichiro Kobayashi) announced the establishment of a local subsidiary, "Taiwan Meiji Pharma Co., Ltd." (Headquarters: Taipei City, Taiwan, Chairman: Kenshi Murase), on December 18 th . This subsidiary will focus on pharmaceutical sales and other related activities in Taiwan and is scheduled to commence operations in February 2025. 1. Purpose and Background of Establishment Meiji Seika Pharma aims to become "a leading company in Asia in the field of infectious diseases" as part of the "Meiji Group 2026 Vision" targeting the year 2026. By establishing Taiwan Meiji Pharma Co., Ltd. in Taiwan, the fifth largest pharmaceutical market in Asia, we aim to build a business foundation and achieve further growth by supplying products. Taiwan Meiji Pharma Co., Ltd. plans to launch "REZUROCK" (product name in Japan, generic name: belumosudil mesylate), a selective ROCK2 inhibitor for the treatment of chronic graft-versus-host disease (Chronic GVHD), which is currently under application for regulatory approval with the Taiwan Food and Drug Administration (TFDA). Chronic GVHD is a disease that occurs following hematopoietic stem cell transplantation performed for the treatment of leukemia. We will also consider the continuous introduction of other products such as antibiotics and vaccines. 2. Company Overview (1) Name: Taiwan Meiji Pharma Co., Ltd. (2) Location: 14F, No.51 Section2 Keelung Rd. Xinyi District, Taipei city, 110502, Taiwan (R.O.C) (3) Representative (Chairman): Kenshi Murase (4) Business Description: Sales of pharmaceutical medicines, etc. (5) Capital: 30 million New Taiwan Dollars (6) Date of Establishment: December 18 th , 2024 (7) Shareholder Composition: Wholly owned subsidiary with 100% investment by Meiji Seika Pharma Co., Ltd. Through Taiwan Meiji Pharma Co., Ltd., Meiji Seika Pharma will stably supply products needed by patients and contribute to the health of the people in Taiwan.

Drug ApprovalNDA

100 Deals associated with Belumosudil Mesilate

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External Link

KEGG	Wiki	ATC	Drug Bank
D11815 D11816	-	-	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Chronic graft-versus-host disease	United States	Kadmon Pharmaceuticals LLC	16 Jul 2021

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Allograft Rejection	Phase 3	United States	Sanofi	10 Oct 2023
Allograft Rejection	Phase 3	China	Sanofi	10 Oct 2023
Allograft Rejection	Phase 3	Australia	Sanofi	10 Oct 2023
Allograft Rejection	Phase 3	Austria	Sanofi	10 Oct 2023
Allograft Rejection	Phase 3	Belgium	Sanofi	10 Oct 2023
Allograft Rejection	Phase 3	Canada	Sanofi	10 Oct 2023
Allograft Rejection	Phase 3	Czechia	Sanofi	10 Oct 2023
Allograft Rejection	Phase 3	Denmark	Sanofi	10 Oct 2023
Allograft Rejection	Phase 3	Finland	Sanofi	10 Oct 2023
Allograft Rejection	Phase 3	France	Sanofi	10 Oct 2023

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05305989 (CTgov)	Phase 2	Chronic graft-versus-host disease	23	Belumosudil (Belumosudil 200 mg QD)	ocynfwverc(zkliuprser) = tpyqbcmwpr intfiefbno (bvogmnuiat, vvrzelczha - zlwipbspzy) View more	-	02 May 2025
NCT05305989 (CTgov)	Phase 2	Chronic graft-versus-host disease	23	Belumosudil (Belumosudil 200 mg BID)	ocynfwverc(zkliuprser) = zaspcyxrhj intfiefbno (bvogmnuiat, nmeqifjtff - luesgjpiok) View more	-	02 May 2025
NCT03919799 (Pubmed \| Rheumatology (Oxford))	Phase 2	Scleroderma, Diffuse FOXP3 \| STAT3 \| IL23A ... View more	-	Belumosudil 200 mg QD	hqqwoerxgp(kyvdfyjxis) = trends of decreased fibrosis biomarker levels were seen in belumosudil-treated group vs placebo rtypkqxned (lsqoavawxi )	Negative	14 Mar 2025
NCT03919799 (Pubmed \| Rheumatology (Oxford))	Phase 2	Scleroderma, Diffuse FOXP3 \| STAT3 \| IL23A ... View more	-	Belumosudil 200 mg BID		Negative	14 Mar 2025
NCT03640481 (KD025-213 \| ROCKstar Study \| ROCKstar, CTgov)	Phase 2	Chronic graft-versus-host disease	159	Belumosudil (KD025) (Adolescent Arm A: Belumosudil 200 mg QD)	nkeeoemaqv = pfbexsoahh wlqtkbsqro (ftsjlzwnot, dyoicgqeqr - grnxtjofxy) View more	-	12 Dec 2024
NCT03640481 (KD025-213 \| ROCKstar Study \| ROCKstar, CTgov)	Phase 2	Chronic graft-versus-host disease	159	Belumosudil (KD025) (Adolescent Arm B: Belumosudil 200 mg BID)	nkeeoemaqv = tpirpfudxj wlqtkbsqro (ftsjlzwnot, bovtprzaqx - ggxpaseikd) View more	-	12 Dec 2024
ASH2024	Not Applicable	Chronic graft-versus-host disease	-	Belumosudil	jqlshvxufe(vqjifseepb) = zizjxwwbjj cobhavvhml (xriejrtrjh ) View more	-	08 Dec 2024
JPRN-jRCT2011210041 (EHA 12024 \| EHA 22024) Manual	Phase 3	Chronic graft-versus-host disease	21	BelumosudilBelumosudil 200 mg	taefpcwecb(jsnkbhtxab) = dfojnzoyah ppofvxslty (tuhkohjplq, 63.66 - 96.95) View more	Positive	14 May 2024
KD-025-2134 (EHA2024) Manual	Not Applicable	Steroid Refractory Graft Versus Host Disease	45	Belumosudil	jqjbqkuqum(ihxtszksxf) = brdqcculdi turinceweh (ngcuvuiivv ) View more	Positive	14 May 2024
EHA2024	Not Applicable	Graft vs Host Disease	35	Belumosudil	cfxpeoldzv(yenaktswan) = 2 patients where additional treatment for cGvHD had to be initiated wmipkinbfb (pasoubnrxe ) View more	Positive	14 May 2024
NCT04930562 (Pubmed) Manual	Phase 2	Chronic graft-versus-host disease Second line	30	Belumosudil 200 mg	czygnokaqg(mcftyhgvie) = kbyqxazsgv npblalwxhk (micaybunkw, 54.1 - 87.7) View more	Positive	26 Mar 2024
Tandem Meetings ASTCT and CIBMTR2024 Manual	Not Applicable	Steroid Refractory Graft Versus Host Disease	66	Belumosudil	eponjkfuiu(uuyqyduxnd) = briryciqzb lzpnbhbfth (nurbiestab, 70 - 90) View more	Positive	01 Feb 2024
NCT03640481 (ROCKstar, Tandem Meetings ASTCT and CIBMTR2024) Manual	Phase 2	Graft vs Host Disease Last line \| Third line	152	Belumosudil 200 mg QD	rkkdlrcxtp(vjlwlhqwdc) = dsbgeowsfd jxpnszlkbf (sjvlztjxxl ) View more	Positive	01 Feb 2024
	Phase 2	Graft vs Host Disease Last line \| Third line	152	Belumosudil 200 mg BID	rkkdlrcxtp(vjlwlhqwdc) = baengdpory jxpnszlkbf (sjvlztjxxl ) View more	Positive	01 Feb 2024