What should I avoid while taking Belumosudil 200mg tablets?

Take at the same time every day. Belumosudil should be taken with a meal at approximately the same time each day. Take with food. The co-administration of food increases the absorption of belumosudil. (Source: DrugBank, licensed under CC BY-NC 4.0)

Do I need a prescription for Belumosudil 200mg tablets?

Belumosudil 200mg tablets is classified as a Valid as a prescribable product in the UK. However, always consult a pharmacist or doctor before use. (Source: NHS dm+d)

What are the brand names for Belumosudil 200mg tablets?

Belumosudil 200mg tablets is the generic name. It is available under brand names including: Rezurock 200mg tablets. (Source: NHS dm+d — Actual Medicinal Products)

Belumosudil 200mg tablets

Prescription only

Requires a prescription from a doctor or prescriber

Tablet

200mg

Oral

Drugs affecting the immune response

Active ingredients:

Belumosudil

BNF classificationBrowse formulary

Where this medicine sits in the British National Formulary — the UK's standard prescribing reference

BNF 08.02.04

ATC classificationBrowse ATC index

International classification by the WHO, grouping medicines by the organ system they act on

ATC L04AA48

Check interactions for Belumosudil

No active safety alerts

Official documents, adverse reaction reporting, and safety monitoring

Report a side effect

Submit a Yellow Card report to the MHRA

Official medicine documents

Yellow Card

Report side effects (MHRA)

Drug safety updates

MHRA alerts for Belumosudil

Source: MHRA Products DatabaseOGL 3.0

Updated 3 months ago(16 Jan 2026)

Safety monitoring data

Yellow Card reports

MHRA

The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.

View Drug Analysis Profile

Suspected adverse reactions reported for Belumosudil

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Interactive Drug Analysis Profiles for all medicines

Report a side effect

Submit a Yellow Card report to the MHRA

Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.

EudraVigilance

EMA

The European Medicines Agency (EMA) collects suspected adverse reaction reports from across the EU/EEA through the EudraVigilance system. Search for safety data on this medicine.

View EudraVigilance report

Suspected adverse reactions reported for Belumosudil

About EudraVigilance

Learn about EU pharmacovigilance and safety monitoring

EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.

1 branded products available

1 productsShow details

1 products

Possibly available on the UK marketDiscontinuedAvailability per NHS dm+d

MHRA licensed products

View all licensed products for Belumosudil on the MHRA register

Rezurock 200mg tablets

Sanofi

Source: NHS dm+dOGL 3.0

Updated about 1 month ago(1 Mar 2026)

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Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.

NHS prescribing volume and spending trends

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Clinical guidelines and formulary information

British National Formulary

Belumosudil

BNF

Drug monograph — bnf.nice.org.uk

Source: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.

NICE clinical guidance(2)

Belumosudil for treating chronic graft-versus-host disease after 2 or more systemic treatments in people 12 years and over (TA949)

TA949

Technology appraisal

Updated Feb 2024

Ruxolitinib for treating acute graft versus host disease that responds inadequately to corticosteroids in people 12 years and over (TA1054)

TA1054

Technology appraisal

Updated Apr 2025

Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.

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Search for this medicine at major UK pharmacy chains. These links open the retailer's own website — results depend on their current online catalogue.

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Official product databases and supply status monitoring

Shortages info

NHS Specialist Pharmacy Service (SPS)

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Discontinuations & alternatives for Belumosudil

Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. emc (electronic medicines compendium) is operated by Datapharm Ltd. Shortage information sourced from NHS Specialist Pharmacy Service (SPS), sps.nhs.uk.

Codes for healthcare professionals and prescribing systems

Show details

These codes are used by healthcare IT systems and prescribers to identify this medicine.

NHS UK identifiers

SNOMED CT

41441911000001105

dm+d ID

41441911000001105

VTM (Virtual Therapeutic Moiety)

1163572003

VMP (Virtual Medicinal Product)

41441911000001105

BNF code

08020400

International identifiers

ATC code — Anatomical Therapeutic Chemical (WHO)

L04AA48

Browse tools

dm+d Browser

NHSBSA medicines dictionary lookup

SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).

Active and completed clinical studies from ClinicalTrials.gov

Show details

Searching UK clinical trials...

Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.

Pharmacology and chemical data from DrugBank

go.drugbank.com

Key facts

Drug status

Approved

Major interactions

None known

Half-life

19 hours

Mechanism

Chronic graft-versus-host disease (GVHD) is a life-threatening complication of a…

Food interactions

2 warnings

Human targets

2 targets

Data: DrugBank · CC BY-NC 4.0

Pharmacokinetics at a glance

Absorption

64%

Following oral administration, the mean bioavailability of belumosudil is 64% and the median T_max at steady-state is 1.26…

Half-life

19 hours

The mean elimination half-life of belumosudil following oral administration is 19 hours.
[L34749]

Protein binding

99.9%

Belumosudil appears to be extensively protein-bound in plasma - in vitro protein binding to serum albumin and alpha-1-acid glycoprotein was found to be 99.9%…

Volume of distribution

184 L

Following a single oral dose of belumosudil in healthy subjects, the mean geometric volume of distribution was 184 L.
[L34749]

Metabolism

The in vitro metabolism of belumosudil occurs primarily via CYP3A4 and to a lesser extent by CYP2C8, CYP2D6, and UGT1A9.
[L34749]…

Elimination

85%

Belumosudil is eliminated primarily in the feces. Following the administration of a radiolabeled oral dose of belumosudil in healthy subjects,…

Clearance

9.83 L/h

The mean clearance of belumosudil is 9.83 L/h.
[L34749]

Pharmacokinetic data: DrugBank · CC BY-NC 4.0

Status:

Approved

Investigational

Small molecule

About this compound

Belumosudil is used in the treatment of chronic graft-versus-host disease (GVHD) and has been investigated for the treatment of pulmonary arterial hypertension.[A236634] It is an inhibitor of rho-associated coiled-coil-containing protein kinases (ROCK), with significantly more selectivity for ROCK2 as compared to ROCK1 (IC₅₀ 100 nM vs. 3 μM, respectively).[L34749] In the treatment of GVHD, a condition in which donor T-cells begin to attack recipient tissues following allogeneic hematopoeitic stem cell transplantation (HSCT), belumosudil helps to resolve immune dysregulation by shifting the balance between Th17 cells and T-regulatory cells, thereby dampening the inflammatory cascade that can occasionally be fatal.[A236644][L34759]

Belumosudil was first approved by the FDA in July 2021, under the brand name Rezurock, for the treatment of chronic GVHD in patients who have tried and failed at least two prior lines of systemic therapy.[L34754] In July 2022, Belumosudil was approved by Health Canada under the brand name RHOLISTIQ to treat the same condition in adult and pediatric patients 12 years or older.[L42925]

Properties:

solid

Avg. mass: 452.52 Da

DrugBank indication

Belumosudil is indicated for the treatment of chronic graft-versus-host disease (GVHD) in adult and pediatric patients 12 years of age and older following failure of at least two other lines of systemic therapy.
[L34749]

Also known as(119)

Belumosudil

2.7.11.1

KIAA0619

p164 ROCK-2

Rho kinase 2

Rho-associated, coiled-coil-containing protein kinase 2

Rho-associated, coiled-coil-containing protein kinase II

ROCK-II

Dosage forms(2)

Tablet (Oral) — 200 mg

Tablet (Oral) — 200 mg/1

Molecular properties(19)

Drug interactions(656)

Known interactions with other medications. Always consult a healthcare professional.

Afatinib

Unknown severity

DB08916

The serum concentration of Afatinib can be increased when it is combined with Belumosudil.

Check this interaction

Bosutinib

Unknown severity

DB06616

The serum concentration of Bosutinib can be increased when it is combined with Belumosudil.

Check this interaction

Brentuximab vedotin

Unknown severity

DB08870

The serum concentration of Brentuximab vedotin can be increased when it is combined with Belumosudil.

Check this interaction

Colchicine

Unknown severity

DB01394

The serum concentration of Colchicine can be increased when it is combined with Belumosudil.

Check this interaction

Edoxaban

Unknown severity

DB09075

The serum concentration of Edoxaban can be increased when it is combined with Belumosudil.

Check this interaction

Ledipasvir

Unknown severity

DB09027

The serum concentration of Ledipasvir can be increased when it is combined with Belumosudil.

Check this interaction

Naloxegol

Unknown severity

DB09049

The serum concentration of Naloxegol can be increased when it is combined with Belumosudil.

Check this interaction

Pazopanib

Unknown severity

DB06589

The serum concentration of Pazopanib can be increased when it is combined with Belumosudil.

Check this interaction

Prucalopride

Unknown severity

DB06480

The serum concentration of Prucalopride can be increased when it is combined with Belumosudil.

Check this interaction

Ranolazine

Unknown severity

DB00243

The serum concentration of Ranolazine can be increased when it is combined with Belumosudil.

Check this interaction

Silodosin

Unknown severity

DB06207

The excretion of Silodosin can be decreased when combined with Belumosudil.

Check this interaction

Topotecan

Unknown severity

DB01030

The serum concentration of Topotecan can be increased when it is combined with Belumosudil.

Check this interaction

Everolimus

Unknown severity

DB01590

The serum concentration of Everolimus can be increased when it is combined with Belumosudil.

Check this interaction

Rifaximin

Unknown severity

DB01220

The serum concentration of Rifaximin can be increased when it is combined with Belumosudil.

Check this interaction

Eluxadoline

Unknown severity

DB09272

The serum concentration of Eluxadoline can be increased when it is combined with Belumosudil.

Check this interaction

Vincristine

Unknown severity

DB00541

The excretion of Vincristine can be decreased when combined with Belumosudil.

Check this interaction

Doxorubicin

Unknown severity

DB00997

The serum concentration of Doxorubicin can be increased when it is combined with Belumosudil.

Check this interaction

Betrixaban

Unknown severity

DB12364

The serum concentration of Betrixaban can be increased when it is combined with Belumosudil.

Check this interaction

Pitolisant

Unknown severity

DB11642

The serum concentration of Belumosudil can be decreased when it is combined with Pitolisant.

Check this interaction

Folic acid

Moderate

DB00158

Belumosudil may decrease the excretion rate of Folic acid which could result in a higher serum level.

Check this interaction

Pravastatin

Moderate

DB00175

Belumosudil may decrease the excretion rate of Pravastatin which could result in a higher serum level.

Check this interaction

Cladribine

Unknown severity

DB00242

The excretion of Cladribine can be decreased when combined with Belumosudil.

Check this interaction

Conjugated estrogens

Moderate

DB00286

Belumosudil may decrease the excretion rate of Conjugated estrogens which could result in a higher serum level.

Check this interaction

Gefitinib

Moderate

DB00317

Belumosudil may decrease the excretion rate of Gefitinib which could result in a higher serum level.

Check this interaction

Sorafenib

Unknown severity

DB00398

The risk or severity of adverse effects can be increased when Sorafenib is combined with Belumosudil.

Check this interaction

Allopurinol

Moderate

DB00437

Belumosudil may decrease the excretion rate of Allopurinol which could result in a higher serum level.

Check this interaction

Cerivastatin

Moderate

DB00439

Belumosudil may decrease the excretion rate of Cerivastatin which could result in a higher serum level.

Check this interaction

Teniposide

Unknown severity

DB00444

The risk or severity of adverse effects can be increased when Teniposide is combined with Belumosudil.

Check this interaction

Prazosin

Moderate

DB00457

Belumosudil may decrease the excretion rate of Prazosin which could result in a higher serum level.

Check this interaction

Raloxifene

Moderate

DB00481

Belumosudil may decrease the excretion rate of Raloxifene which could result in a higher serum level.

Check this interaction

Celecoxib

Moderate

DB00482

Belumosudil may decrease the excretion rate of Celecoxib which could result in a higher serum level.

Check this interaction

Zidovudine

Unknown severity

DB00495

The risk or severity of adverse effects can be increased when Zidovudine is combined with Belumosudil.

Check this interaction

Oxaliplatin

Unknown severity

DB00526

The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Belumosudil.

Check this interaction

Fluorouracil

Unknown severity

DB00544

The risk or severity of adverse effects can be increased when Fluorouracil is combined with Belumosudil.

Check this interaction

Methotrexate

Unknown severity

DB00563

The risk or severity of adverse effects can be increased when Methotrexate is combined with Belumosudil.

Check this interaction

Ivermectin

Moderate

DB00602

Belumosudil may decrease the excretion rate of Ivermectin which could result in a higher serum level.

Check this interaction

Imatinib

Unknown severity

DB00619

The risk or severity of adverse effects can be increased when Imatinib is combined with Belumosudil.

Check this interaction

Testosterone

Moderate

DB00624

Belumosudil may decrease the excretion rate of Testosterone which could result in a higher serum level.

Check this interaction

Clofarabine

Unknown severity

DB00631

The risk or severity of adverse effects can be increased when Clofarabine is combined with Belumosudil.

Check this interaction

Sumatriptan

Moderate

DB00669

Belumosudil may decrease the excretion rate of Sumatriptan which could result in a higher serum level.

Check this interaction

Tamoxifen

Moderate

DB00675

Belumosudil may decrease the excretion rate of Tamoxifen which could result in a higher serum level.

Check this interaction

Mycophenolate mofetil

Unknown severity

DB00688

The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Belumosudil.

Check this interaction

Daunorubicin

Unknown severity

DB00694

The risk or severity of adverse effects can be increased when Daunorubicin is combined with Belumosudil.

Check this interaction

Nitrofurantoin

Moderate

DB00698

Belumosudil may decrease the excretion rate of Nitrofurantoin which could result in a higher serum level.

Check this interaction

Lamivudine

Moderate

DB00709

Belumosudil may decrease the excretion rate of Lamivudine which could result in a higher serum level.

Check this interaction

Riluzole

Moderate

DB00740

Belumosudil may decrease the excretion rate of Riluzole which could result in a higher serum level.

Check this interaction

Irinotecan

Unknown severity

DB00762

The risk or severity of adverse effects can be increased when Irinotecan is combined with Belumosudil.

Check this interaction

Sulfasalazine

Unknown severity

DB00795

The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Belumosudil.

Check this interaction

Donepezil

Moderate

DB00843

Belumosudil may decrease the excretion rate of Donepezil which could result in a higher serum level.

Check this interaction

Ezetimibe

Moderate

DB00973

Belumosudil may decrease the excretion rate of Ezetimibe which could result in a higher serum level.

Check this interaction

Showing 50 of 656 interactions

Food & lifestyle interactions

Advice

Take at the same time every day. Belumosudil should be taken with a meal at approximately the same time each day.

Take With Food

Take with food. The co-administration of food increases the absorption of belumosudil.

Toxicity & overdose

There are no data regarding overdosage with belumosudil.

How it works

Mechanism of action

Chronic graft-versus-host disease (GVHD) is a life-threatening complication of allogeneic hematopoietic stem cell transplantation in which the transplanted donor T-cells recognize the recipient's tissues as foreign and mount an immune response.[A236639] During the conditioning regimen prior to stem cell transplantation (e.g. involving irradiation or chemotherapy) the host tissues can become damaged which results in downstream inflammatory responses and the generation of inflammatory mediators like TNF-alpha and IL-1. These cytokines increase the expression of host major histocompatibility (MHC) antigens and adhesion molecules which enhances the ability of mature donor T-cells to recognize these molecules. The activation of these donor T-cells results in the activation of mononuclear phagocytes, whose effector functions are triggered by stimulatory molecules generated by the damage incurred during the conditioning phase of treatment. Activated macrophages and cytotoxic T-lymphocytes begin to directly lyse target cells and/or cause their apoptosis, which eventually leads to local tissue damage and further inflammatory responses.[A236644]

Belumosudil is an inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2), a protein that plays a vital role in the pathogenesis of immune and fibrotic diseases. The inhibition of ROCK2 has been shown to resolve immune dysregulation by down-regulating pro-inflammatory Th17 cells and up-regulating regulatory T-cells by manipulating the phosphorylation of STAT3 and STAT5.[L34749][L34759]

Pharmacodynamics

Belumosudil appears to inhibit several pro-fibrotic and pro-inflammatory processes in order to prevent and treat the damage incurred by graft-versus-host disease. Given its mechanism of action and findings in animal trials, belumosudil is considered to carry embryo-fetal toxicity and may cause significant harm to a developing fetus should a pregnant mother be exposed.[L34749] Female patients of reproductive potential, or male patients with female partners of reproductive potential, should be advised to use effective contraception during treatment with belumosudil and for one week after the last dose.[L34749]

Pharmacokinetics

How the body processes this drug — absorption, distribution, metabolism, and elimination

Absorption

Following oral administration, the mean bioavailability of belumosudil is 64% and the median T_max at steady-state is 1.26 to 2.53 hours.
[L34749]
As compared to administration in a fasted state, belumosudil C_max and AUC increased by 2.2 and 2 times, respectively, when administered with a high-fat, high-calorie meal.
[L34749]

Half-life

The mean elimination half-life of belumosudil following oral administration is 19 hours.
[L34749]

Protein binding

Belumosudil appears to be extensively protein-bound in plasma - in vitro protein binding to serum albumin and alpha-1-acid glycoprotein was found to be 99.9% and 98.6%, respectively.
[L34749]

Volume of distribution

Following a single oral dose of belumosudil in healthy subjects, the mean geometric volume of distribution was 184 L.
[L34749]

Metabolism

The in vitro metabolism of belumosudil occurs primarily via CYP3A4 and to a lesser extent by CYP2C8, CYP2D6, and UGT1A9.
[L34749]
The specific metabolites generated by belumosudil metabolism remain unclear.

Route of elimination

Belumosudil is eliminated primarily in the feces. Following the administration of a radiolabeled oral dose of belumosudil in healthy subjects, approximately 85% of the radioactivity was recovered in the feces, 30% of which was unchanged parent drug, with less than 5% recovered in the urine.
[L34749]

Clearance

The mean clearance of belumosudil is 9.83 L/h.
[L34749]

Drug targets(2)

Proteins and enzymes this drug interacts with in the body

Rho-associated protein kinase 2

BE0004191

ROCK2

inhibitor

Specific functionATP binding

Cellular location

Cytoplasm

General function & pharmacology

Protein kinase which is a key regulator of actin cytoskeleton and cell polarity. Involved in regulation of smooth muscle contraction, actin cytoskeleton organization, stress fiber and focal adhesion formation, neurite retraction, cell adhesion and motility via phosphorylation of ADD1, BRCA2, CNN1, EZR, DPYSL2, EP300, MSN, MYL9/MLC2, NPM1, RDX, PPP1R12A and VIM. Phosphorylates SORL1 and IRF4.

Acts as a negative regulator of VEGF-induced angiogenic endothelial cell activation. Positively regulates the activation of p42/MAPK1-p44/MAPK3 and of p90RSK/RPS6KA1 during myogenic differentiation. Plays an important role in the timely initiation of centrosome duplication.

Inhibits keratinocyte terminal differentiation. May regulate closure of the eyelids and ventral body wall through organization of actomyosin bundles. Plays a critical role in the regulation of spine and synaptic properties in the hippocampus.

Plays an important role in generating the circadian rhythm of the aortic myofilament Ca(2+) sensitivity and vascular contractility by modulating the myosin light chain phosphorylation

Rho-associated protein kinase 1

BE0001016

ROCK1

inhibitor

Specific functionATP binding

Cellular location

Cytoplasm

General function & pharmacology

Protein kinase which is a key regulator of the actin cytoskeleton and cell polarity .
PMID:10436159 PMID:10652353 PMID:11018042 PMID:11283607 PMID:17158456 PMID:18573880 PMID:19131646 PMID:8617235 PMID:9722579

Involved in regulation of smooth muscle contraction, actin cytoskeleton organization, stress fiber and focal adhesion formation, neurite retraction, cell adhesion and motility via phosphorylation of DAPK3, GFAP, LIMK1, LIMK2, MYL9/MLC2, TPPP, PFN1 and PPP1R12A .
PMID:10436159 PMID:10652353 PMID:11018042 PMID:11283607 PMID:17158456 PMID:18573880 PMID:19131646 PMID:23093407 PMID:23355470 PMID:8617235 PMID:9722579

Phosphorylates FHOD1 and acts synergistically with it to promote SRC-dependent non-apoptotic plasma membrane blebbing .
PMID:18694941
Phosphorylates JIP3 and regulates the recruitment of JNK to JIP3 upon UVB-induced stress .
PMID:19036714
Acts as a suppressor of inflammatory cell migration by regulating PTEN phosphorylation and stability (By similarity). Acts as a negative regulator of VEGF-induced angiogenic endothelial cell activation .
PMID:19181962
Required for centrosome positioning and centrosome-dependent exit from mitosis (By similarity). Plays a role in terminal erythroid differentiation .
PMID:21072057
Inhibits podocyte motility via regulation of actin cytoskeletal dynamics and phosphorylation of CFL1 (By similarity).

Promotes keratinocyte terminal differentiation .
PMID:19997641
Involved in osteoblast compaction through the fibronectin fibrillogenesis cell-mediated matrix assembly process, essential for osteoblast mineralization (By similarity). May regulate closure of the eyelids and ventral body wall by inducing the assembly of actomyosin bundles (By similarity)

Metabolizing enzymes(7)

Enzymes involved in drug metabolism — important for understanding drug interactions

Enzyme activity key

substrate

inhibitor

inducer

CYP3A4Cytochrome P450 3A4

substrate

CYP2C8Cytochrome P450 2C8

substrate

CYP2D6Cytochrome P450 2D6

substrate

inhibitor

UGT1A9UDP-glucuronosyltransferase 1A9

substrate

inhibitor

CYP1A2Cytochrome P450 1A2

inhibitor

CYP2C19Cytochrome P450 2C19

inhibitor

UGT1A1UDP-glucuronosyltransferase 1A1

inhibitor

Transporters(3)

Proteins that transport this drug across cell membranes

ATP-dependent translocase ABCB1

BE0001032

ABCB1

substrate

inhibitor

Specific functionABC-type xenobiotic transporter activity

Cellular location

Cell membrane

General function & pharmacology

Translocates drugs and phospholipids across the membrane .
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548

Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218

Broad substrate specificity ATP-binding cassette transporter ABCG2

BE0001067

ABCG2

inhibitor

Specific functionABC-type xenobiotic transporter activity

Cellular location

Cell membrane

General function & pharmacology

Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells .
PMID:11306452 PMID:12958161 PMID:19506252 PMID:20705604 PMID:28554189 PMID:30405239 PMID:31003562

Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme .
PMID:20705604 PMID:23189181
Also mediates the efflux of sphingosine-1-P from cells .
PMID:20110355
Acts as a urate exporter functioning in both renal and extrarenal urate excretion .
PMID:19506252 PMID:20368174 PMID:22132962 PMID:31003562 PMID:36749388

In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates .
PMID:12682043 PMID:28554189 PMID:30405239

Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity).

Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux .
PMID:11306452 PMID:12477054 PMID:15670731 PMID:18056989 PMID:31254042

In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).

In inflammatory macrophages, exports itaconate from the cytosol to the extracellular compartment and limits the activation of TFEB-dependent lysosome biogenesis involved in antibacterial innate immune response

Solute carrier organic anion transporter family member 1B1

BE0001004

SLCO1B1

inhibitor

Specific functionbile acid transmembrane transporter activity

Cellular location

Basolateral cell membrane

General function & pharmacology

Mediates the Na(+)-independent uptake of organic anions .
PMID:10358072 PMID:15159445 PMID:17412826

Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (dehydroepiandrosterone 3-sulfate, 17-beta-glucuronosyl estradiol, and estrone 3-sulfate), as well as eicosanoids (prostaglandin E2, thromboxane B2, leukotriene C4, and leukotriene E4), and thyroid hormones (T4/L-thyroxine, and T3/3,3',5'-triiodo-L-thyronine) .
PMID:10358072 PMID:10601278 PMID:10873595 PMID:11159893 PMID:12196548 PMID:12568656 PMID:15159445 PMID:15970799 PMID:16627748 PMID:17412826 PMID:19129463 PMID:26979622

Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop .
PMID:22232210
Involved in the clearance of endogenous and exogenous substrates from the liver .
PMID:10358072 PMID:10601278
Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition .
PMID:26383540
May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier (Probable). Can transport HMG-CoA reductase inhibitors (also known as statins), such as pravastatin and pitavastatin, a clinically important class of hypolipidemic drugs .
PMID:10601278 PMID:15159445 PMID:15970799

May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drug methotrexate .
PMID:23243220
May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver .
PMID:16624871 PMID:16627748
Shows a pH-sensitive substrate specificity towards prostaglandin E2 and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment .
PMID:19129463
Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions PMID:19129463

Carriers(2)

Proteins that carry this drug through the body

Albumin

BE0000530

ALB

binder

Specific functionantioxidant activity

Cellular location

Secreted

General function & pharmacology

Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc .
PMID:19021548
Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity).

Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity).

Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli .
PMID:6234017
Does not prevent iron uptake by the bacterial siderophore aerobactin PMID:6234017

Alpha-1-acid glycoprotein 1

BE0000925

ORM1

binder

Cellular location

Secreted

General function & pharmacology

Functions as a transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body.

Appears to function in modulating the activity of the immune system during the acute-phase reaction

Scientific references(4)

Cutler C.S., Lee S.J., Arai S., Rotta M., Zoghi B., Lazaryan A., Ramakrishnan A., DeFilipp Z., Salhotra A., Chai-Ho W., Mehta R.S., Wang T., Arora M., Pusic I., Saad A., Shah N.N., Abhyankar S., Bachier C., Galvin J.P., Im A., Langston A., Liesveld J.L., Juckett M., Logan A., Schachter L., Alavi A., Howard D.S., Waksal H., Ryan J., Eiznhamer D., Aggarwal S.K., Ieyoub J., Schueller O., Green L.S., Yang Z., Krenz H., Jagasia M., Blazar B.R., Pavletic S.Z.

Belumosudil for Chronic Graft-versus-Host Disease (cGVHD) After 2 or More Prior Lines of Therapy: The ROCKstar Study. Blood. 2021 Jul 15. pii: 476399. doi: 10.

1182/blood

2021012021

PMID: 34265047 DOI: 10.1182/blood.2021012021

Braun L.M., Zeiser R.

Immunomodulatory Therapies for the Treatment of Graft-versus-host Disease.

Hemasphere

2021 Jun 15(6):e581. doi: 10.1097/HS9.0000000000000581. eCollection 2021 Jun

PMID: 34095764 DOI: 10.1097/HS9.0000000000000581

Ferrara J.L., Reddy P.

Pathophysiology of graft-versus-host disease.

Semin Hematology

2006 Jan43(1):3-10. doi: 10.1053/j.seminhematol.2005.09.001

PMID: 16412784 DOI: 10.1053/j.seminhematol.2005.09.001

Yamamura A., Nayeem M.J., Sato M.

The Rho kinase 2 (ROCK2)-specific inhibitor KD025 ameliorates the development of pulmonary arterial hypertension.

Biochemistry Biophys Research Communications

2021 Jan 1534:795-801. doi: 10.1016/j.bbrc.2020.10.106. Epub 2020 Nov 5

PMID: 33160621 DOI: 10.1016/j.bbrc.2020.10.106

ATC classification(1 code)

ATC L04AA48

Affected organisms(1)

Humans and other mammals

International brands(1)

Salt forms(2)

Belumosudil mesylate(DBSALT003188)

Belumosudil trifluoroacetate(DBSALT003189)

Experimental properties(2)

Protein Data Bank entries(1)

7z39

Commercial products(3)

Chemical identifiers

CAS, UNII, InChI Key and database cross-references

Show

Linked compound data from DrugBank Open Data (CC BY-NC 4.0)

Belumosudil

DB16703

CAS number

911417-87-3

UNII (FDA)

834YJF89WO

InChI Key (molecular fingerprint)

GKHIVNAUVKXIIY-UHFFFAOYSA-N

Additional database identifiers

Drugs Product Database (DPD)

23710

KEGG Drug

D11815

ChemSpider

10124479

BindingDB

322155

PDB

ICQ

Wikipedia

Belumosudil

ChEMBL

CHEMBL2005186

ZINC

ZINC000063298464

RxCUI

2564025

HUGO Gene Nomenclature Committee (HGNC)

HGNC:10252

GeneCards

ROCK2

GenBank Gene Database

D87931

GenBank Protein Database

4520225

Guide to Pharmacology

1504

UniProtKB

O75116

UniProt Accession

ROCK2_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:10251

GenAtlas

ROCK1

GeneCards

ROCK1

GenBank Gene Database

U43195

GenBank Protein Database

1276901

Guide to Pharmacology

1503

UniProtKB

Q13464

UniProt Accession

ROCK1_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:2637

GenAtlas

CYP3A4

GeneCards

CYP3A4

GenBank Gene Database

M18907

Guide to Pharmacology

1337

UniProtKB

P08684

UniProt Accession

CP3A4_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:2622

GenAtlas

CYP2C8

GeneCards

CYP2C8

GenBank Gene Database

M17397

Guide to Pharmacology

1325

UniProtKB

P10632

UniProt Accession

CP2C8_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:2625

GenAtlas

CYP2D6

GeneCards

CYP2D6

GenBank Gene Database

M20403

GenBank Protein Database

181350

Guide to Pharmacology

1329

UniProtKB

P10635

UniProt Accession

CP2D6_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:12541

GeneCards

UGT1A9

GenBank Gene Database

S55985

GenBank Protein Database

7690346

UniProtKB

O60656

UniProt Accession

UD19_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:2596

GenAtlas

CYP1A2

GeneCards

CYP1A2

GenBank Gene Database

Z00036

Guide to Pharmacology

1319

UniProtKB

P05177

UniProt Accession

CP1A2_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:2621

GeneCards

CYP2C19

GenBank Gene Database

M61854

GenBank Protein Database

181344

Guide to Pharmacology

1328

UniProtKB

P33261

UniProt Accession

CP2CJ_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:12530

GeneCards

UGT1A1

GenBank Gene Database

M57899

GenBank Protein Database

184473

Guide to Pharmacology

2990

UniProtKB

P22309

UniProt Accession

UD11_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:399

GenAtlas

ALB

GeneCards

ALB

GenBank Gene Database

V00494

GenBank Protein Database

28590

UniProtKB

P02768

UniProt Accession

ALBU_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:8498

GenAtlas

ORM1

GeneCards

ORM1

GenBank Gene Database

X02544

GenBank Protein Database

757907

UniProtKB

P02763

UniProt Accession

A1AG1_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:40

GenAtlas

ABCB1

GeneCards

ABCB1

GenBank Gene Database

M14758

GenBank Protein Database

307180

Guide to Pharmacology

768

UniProtKB

P08183

UniProt Accession

MDR1_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:74

GenAtlas

ABCG2

GeneCards

ABCG2

GenBank Gene Database

AF103796

GenBank Protein Database

4185796

Guide to Pharmacology

792

UniProtKB

Q9UNQ0

UniProt Accession

ABCG2_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:10959

GenAtlas

SLCO1B1

GeneCards

SLCO1B1

GenBank Gene Database

AF060500

GenBank Protein Database

5051630

Guide to Pharmacology

1220

UniProtKB

Q9Y6L6

UniProt Accession

SO1B1_HUMAN

Patent information

6 active patents

12097202

United States

Approved 24 Sept 2024 · Expires 14 Jul 2042

16y 3m

11311541

United States

Approved 26 Apr 2022 · Expires 9 Apr 2035

9 years

10696660

United States

Approved 30 Jun 2020 · Expires 7 Oct 2033

7y 6m

10183931

United States

Approved 22 Jan 2019 · Expires 7 Oct 2033

7y 6m

9815820

United States

Approved 14 Nov 2017 · Expires 7 Oct 2033

7y 6m

Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.

DrugBank citations

If you use DrugBank data in your research, please cite the following publications:

Knox C., Wilson M., Klinger C.M., et al

DrugBank 6.

0: the DrugBank Knowledgebase for 2024

Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275

PMID: 37953279

Wishart D.S., Feunang Y.D., Guo A.C., et al

DrugBank 5.

0: a major update to the DrugBank database for 2018

Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082

PMID: 29126136

Show earlier publications

Law V., Knox C., Djoumbou Y., et al

DrugBank 4.

0: shedding new light on drug metabolism

Nucleic Acids Res. 2014 Jan 142(1):D1091-7

PMID: 24203711

Knox C., Law V., Jewison T., et al

DrugBank 3.

0: a comprehensive resource for 'omics' research on drugs

Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41

PMID: 21059682

Wishart D.S., Knox C., Guo A.C., et al

DrugBank: a knowledgebase for drugs, drug actions and drug targets.

Nucleic Acids Research

2008 Jan36(Database issue):D901-6

PMID: 18048412

Wishart D.S., Knox C., Guo A.C., et al

DrugBank: a comprehensive resource for in silico drug discovery and exploration.

Nucleic Acids Research

2006 Jan 134(Database issue):D668-72

PMID: 16381955

Source: go.drugbank.comCC BY-NC 4.0

Updated 30 days ago(4 Mar 2026)

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