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Belumosudil

  • Prescription medicine
  • Prescription only
  • Identity checked
  • Sources last checked 2026-09-04

This page shows what was measured, who it was measured in, and what that does not settle.

What Belumosudil does in the body

REZUROCK is indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy.

From the FDA-approved label: Belumosudil is an inhibitor of rho-associated, coiled-coil containing protein kinase (ROCK) which inhibits ROCK2 and ROCK1 with IC 50 values of approximately 100 nM and 3 µM, respectively. Belumosudil down-regulated proinflammatory responses via regulation of STAT3/STAT5 phosphorylation and shifting Th17/Treg balance in ex-vivo or in vitro -human T cell assays. Belumosudil also inhibited aberrant pro-fibrotic signaling, in vitro . In vivo , belumosudil demonstrated activity in animal models of chronic GVHD.

Why people take it. REZUROCK is indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy.

What happened in people

RNAWiki has not yet published a reviewed conclusion for this use.

A fixed RNAWiki sentence

Where this came from

Wording RNAWiki always uses, not a finding about this substance.

No reviewed claim names a result for any goal on this record.

No source is stored against this line.

The limit that matters most

Not recorded.

Where it acts
Not recorded.
Kind of result
No result is published, so no kind of result applies yet
Supervision
Professional supervision is normally required. A regulator classifies this substance in a way that restricts how it is supplied.

What the registries record it as

  • The substance registry classes this as chemical.

    FDA substance registry · 834YJF89WO · read 2026-08-29

  • Its recorded molecular formula is C27H28N6O5S, weighing 548.62 g/mol.

    US prescribing information · 102e4ef4-7f84-4e34-8df1-479c24d1575d · read 2026-08-30

Where each sentence above came from

The use the label states, quoted from it. No plain-language version of this sentence has been written.

The use the label states, quoted from it. It is written for a clinician, not for a reader without medical training.

No statement of the main limit is recorded.

The four opening statements run to 150 words.

Words this page uses

Four words worth knowing first

Chosen from what this page shows, with each one explained before the word it depends on.

Biomarker

A biomarker is a number from a test that stands in for something about health.

A picture of it, and where the picture fails

A biomarker is like a fuel gauge.

Where that stops being true. A gauge is wired to the tank. Many biomarkers are only loosely tied to health.

What people get wrong. A better number is read as a better life. Several medicines improved a number and helped nobody.

A measurable indicator used as a substitute for a clinical outcome of interest.

Placebo

A placebo is a dummy treatment given so the real one can be compared with it.

A picture of it, and where the picture fails

A placebo is like a blank control in an experiment.

Where that stops being true. A blank does nothing. People given a placebo often do get better.

What people get wrong. A placebo effect is read as imaginary. The improvement is measured and real.

An inactive intervention matched in appearance to the test intervention, used to control for non-specific effects.

Comparator

A comparator is whatever the treatment was measured against.

A picture of it, and where the picture fails

It is like the other runner in a race.

Where that stops being true. A race has one winner. A study can show both arms improved.

What people get wrong. Results are read without asking what the other group got. Beating nothing is not beating a treatment.

The control condition against which the experimental intervention is assessed.

What happened in peopleRead from sources, not yet reviewed

What happened in people

Each card is one study: the exact question it asked, who was in it, and whether it showed what it set out to show.

Overall response rate

The study did not show it

Who was studied
NCT07771439
How many people
356
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.

The limits of this study, and where it came from

Main limit. No limitation is recorded for this study.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

Event-Free Survival (EFS)

The study did not show it

Who was studied
NCT06143891
How many people
260
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
Living longer, or avoiding a major event
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.

The limits of this study, and where it came from

Main limit. No limitation is recorded for this study.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

Part 1 (dose finding, experimental substudies): Determination of recommended dose of novel agents in combination with isatuximab

The study did not show it

Who was studied
NCT04643002
How many people
258
Study design
Phase 1/Phase 2
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.

The limits of this study, and where it came from

Main limit. No limitation is recorded for this study.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

Time from randomization to the first occurrence of probable or definite CLAD (per ISHLT 2019 standard defined criteria), lung retransplant, or death

The study did not show it

Who was studied
NCT06476132
How many people
234
Study design
Phase 2
Compared against
Not recorded for this study
Kind of result
Living longer, or avoiding a major event
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.

The limits of this study, and where it came from

Main limit. No limitation is recorded for this study.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

Percent change from baseline to Week 26 in forced expiratory volume in 1 second (FEV1)

The study did not show it

Who was studied
NCT06082037
How many people
180
Study design
Phase 3
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.

The limits of this study, and where it came from

Main limit. No limitation is recorded for this study.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot

Overall Response Rate (ORR)

The study did not show it

Who was studied
NCT03640481
How many people
159
Study design
Phase 2
Compared against
Not recorded for this study
Kind of result
A number that stands in for health
What was found
Result not recorded on this page
Repeated elsewhere
Unreplicated

What this does not prove. A study that did not show an effect does not show that no effect exists anywhere.

The limits of this study, and where it came from

Main limit. No limitation is recorded for this study.

How far it carries. This study is recorded from the curated record, not from the registry match.

Form and route. Oral

Interval reported. Not recorded in this summary

Written into the record, not signed off as a reviewed claim.

  • openFDA Drugs@FDA · a recorded source, not a stored snapshot
  • openFDA NDC Directory · a recorded source, not a stored snapshot
  • openFDA SPL label · a recorded source, not a stored snapshot
  • PubChem PUG-REST · a recorded source, not a stored snapshot
What we know
RNAWiki holds 6 written-up human studies for this substance, each with the question it asked.
How we know it
Each card names the study, the number of people and what the study set out to measure.
What this does not prove
These summaries were written by a person and have not been signed off as reviewed claims.
Why it matters
A study that failed is as informative as one that worked, and both are here.
What we still do not know
No reviewed claim exists, so no exact population, effect size or interval is published yet.

What is missing or unclearRead from sources, not yet reviewed

Were people like you studied?

RNAWiki cannot tell whether a study fits you. It can show who was in it, and where the result stops carrying.

Who was studied

People similar to this profile were included.

  • REZUROCK is indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy.

Who is missing from the studies

  • Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

What the label states about particular groups

  • On pediatric, the label states: “The safety and effectiveness of REZUROCK in pediatric patients less than 12 years old have not been established.”

    US prescribing information · 102e4ef4-7f84-4e34-8df1-479c24d1575d · read 2026-08-30

  • On older people, the label states: “Of the 186 patients with chronic GVHD in clinical studies of REZUROCK, 26% were 65 years and older.”

    US prescribing information · 102e4ef4-7f84-4e34-8df1-479c24d1575d · read 2026-08-30

  • On people who are pregnant, the label states: “Risk Summary Based on findings from animal studies and the mechanism of action [see Clinical Pharmacology (12.1) ] , REZUROCK can cause fetal harm when administered to pregnant women.”

    US prescribing information · 102e4ef4-7f84-4e34-8df1-479c24d1575d · read 2026-08-30

  • On people who are breastfeeding, the label states: “Risk Summary There are no data available on the presence of belumosudil or its metabolites in human milk or the effects on the breastfed child, or milk production.”

    US prescribing information · 102e4ef4-7f84-4e34-8df1-479c24d1575d · read 2026-08-30

  • On people with reduced liver function, the label states: “Avoid use in patients with moderate hepatic impairment (Child-Pugh B) or severe hepatic impairment (Child-Pugh C) without liver GVHD [see Dosage and Administration (2.4) , Clinical Pharmacology (12.3) ] .”

    US prescribing information · 102e4ef4-7f84-4e34-8df1-479c24d1575d · read 2026-08-30

  • On people with reduced kidney function, the label states: “Treatment with REZUROCK has not been studied in patients with pre-existing severe renal impairment.”

    US prescribing information · 102e4ef4-7f84-4e34-8df1-479c24d1575d · read 2026-08-30

Where the result stopped carrying

  • This is a scope explorer, not a diagnosis engine.
  • It shows who was studied so you can see whether people similar to you were included.

RNAWiki cannot tell whether a study fits you. It can show who was in it.

What it would be like to takeRead from sources, not yet reviewed

Why it might seem to do nothing

A real effect and a noticed effect are different things. These are the recorded reasons the two come apart.

It was studied in different people

The people in the studies were not much like the reader.

On this record: Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

The evidence may simply be wrong

Small early studies often do not hold up.

On this record: RNAWiki has not yet published a reviewed conclusion for this use.

Other reasons RNAWiki checked and found nothing for (11)
It was studied for a different goal
The studies measured something else entirely. Nothing in this record points to this reason.
A different form was studied
The studied form is not the form on the shelf. Nothing in this record points to this reason.
There was nothing to correct
Where a level is already normal, topping it up may change nothing. Nothing in this record points to this reason.
Something else had to happen too
In the studies it was paired with training, a diet or another treatment. Nothing in this record points to this reason.
The change is too small to feel
A real change can still sit below what a person notices. Nothing in this record points to this reason.
Day-to-day swing hides it
Sleep, food, stress and time of day move most numbers more than this would. Nothing in this record points to this reason.
Not enough time yet
The studies ran longer than the person has waited. Nothing in this record points to this reason.
It was not taken as studied
Missed days change the result, and studies count them. Nothing in this record points to this reason.
Something else changed at the same time
Two changes at once cannot be told apart afterwards. Nothing in this record points to this reason.
The product may not be what it says
Contents of a sold product are not always what the label states. Nothing in this record points to this reason.
No recorded reason
RNAWiki has nothing stored that would explain it. Nothing in this record points to this reason.

None of these is a reason to take more. Taking more is not a step this page ever suggests.

What it would be like to takeRead from sources, not yet reviewed

What taking it involves

The recorded facts about getting hold of it and using it. Nothing here is a suggestion about what you should do.

How it is supplied

Prescription only

Quoted from a source

Where this came from

Copied from a source RNAWiki stored, with the source named.

Read from the recorded approval status.

No source is stored against this line.

Form and route

Oral

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

The form and route recorded on this substance.

No source is stored against this line.

Who oversees it

Professional supervision is normally required. A regulator classifies this substance in a way that restricts how it is supplied.

Quoted from a source

Where this came from

Copied from a source RNAWiki stored, with the source named.

Suppression classes recorded: S1, S3.

No source is stored against this line.

What is in the pack

Sold as tablet, given by the oral route.

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

Recorded notes on how this is sold and what that means for what is in the pack.

No source is stored against this line.

Where it is registered

Regulatory records are listed in the technical disclosure at the foot of this page.

Counted from records

Where this came from

A count of rows RNAWiki holds. It describes our records, not your body.

Register entries are stored per jurisdiction and shown with their dates.

No source is stored against this line.

Why people stop

Not recorded.

Nothing recorded

Where this came from

RNAWiki holds nothing here and says so rather than guessing.

No record of why people stopped taking it is stored for this substance.

No source is stored against this line.

What it would be like to takeNothing found in the sources checked

What can go wrong

Sorted by where each line came from. A regulator's label and a report somebody sent in are not the same kind of fact.

Nothing found in the sources checked

No harm is recorded against this substance in the sources RNAWiki checked. Finding nothing is not the same as showing there is nothing.

The sources listed were searched and held nothing. That is not the same as nothing existing.

Over a long time. No completed tested study window is recorded, so long-term effects are not established by the registry record.

Groups the studies covered thinly. Which groups were under-represented in the studies has not been recorded for this substance. Pregnancy, breastfeeding, children, older adults, and people with liver or kidney conditions are commonly excluded from trials; nothing here says whether they were.

What is missing or unclearRead from sources, not yet reviewed

Does the exact form matter?

Evidence belongs to the exact thing that was tested. A different salt, a different mixture or a different preparation is a different question.

The form that was studied

Oral

Source-linked record

Where this came from

A person wrote this into the record with the study named beside it. No reviewer has signed it off.

The form used in the studies cited on this page.

No source is stored against this line.

What is sold

Not recorded.

Nothing recorded

Where this came from

RNAWiki holds nothing here and says so rather than guessing.

Nothing further is recorded about which forms are sold.

No source is stored against this line.

What is recorded as being sold

  • 6 products list this as an active ingredient in the United States drug directory. 6 of them contain it and nothing else.

    FDA National Drug Code directory · 50379-0028 · read 2026-08-29

  • They are sold as powder and tablet, taken oral.

    FDA National Drug Code directory · 50379-0028 · read 2026-08-29

  • 1 published label names it as an active ingredient. 1 of them describe this substance alone, which is where its own label text on this page comes from.

    US prescribing information · 102e4ef4-7f84-4e34-8df1-479c24d1575d · read 2026-08-29

  • Those labels are classed as human prescription drug.

    US prescribing information · 102e4ef4-7f84-4e34-8df1-479c24d1575d · read 2026-08-29

  • Rezurock is oral at 3 DOSAGE FORMS AND STRENGTHS Each 200 mg belumosudil tablet is a pale yellow film-coated oblong tablet debossed with "KDM" on one side and "200" on the other side., recorded as fda label in effect 2026-04-07 in the United States.

    US prescribing information · 102e4ef4-7f84-4e34-8df1-479c24d1575d · read 2026-08-30

Evidence carries across two names for one substance. It does not carry across a salt, a mirror form or a mixture.

What it would be like to takeRead from sources, not yet reviewed

What you could measure

This one is decided with a clinician, so this section holds questions to ask rather than a plan to run.

Self-experiment planning is not offered for a prescription or clinician-supervised medicine. The questions below are for a clinician or pharmacist.

Questions worth asking

  • Which of the trials of Belumosudil studied people like me?
  • What was measured, and for how long?
  • Was the result a laboratory value or a health outcome?
  • What would we watch for, and when would we stop?

Tracking can show whether something changed for you. It cannot show what caused it.

RNAWiki records evidence. It does not say whether this substance is right for you.

What is missing or unclearRead from sources, not yet reviewed

What nobody knows yet

Open questions, each with why it is open and what would close it.

Missing populations

Which groups were under-represented in the studies has not been recorded.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Missing long-term data

No completed tested study window is recorded.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

No reviewed conclusion

RNAWiki has not yet published a reviewed conclusion for this use.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Missing interaction studies

No interaction was found in the registers checked. Not finding one is not the same as showing there is none.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Formulation uncertainty

Several salts, forms or products of Belumosudil are recorded. Results from one form may not transfer to another.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

Mechanism not reviewed

No reviewed mechanism story exists for this substance.

Why it matters. Recorded by the evidence model as a gap on this record.

What would answer it

A study that measures it, and a reviewer to sign it off.

Last checked 2026-09-04. Searched: The sources listed in the receipts at the foot of this page.

What happened in peopleRead from sources, not yet reviewed

Check any of this yourself

Every line above traced back to the study it came from. This is the technical layer, and the vocabulary changes here.

Where else this substance is registered

FDA substance identifier (UNII)
834YJF89WO
RxNorm concept
2564031

Checks this page had to pass

  • Passed

    Identity resolved

    no open identity hold

  • Passed

    No unresolved merge across substance families

    no quarantine open

  • Passed

    Every public sentence names a source

    The opening statement carries the origin: Quoted from a stored source.

  • Not passed

    Trial roles classified for highlighted evidence

    No registered study is classified as testing this substance.

  • Passed

    No internal keys in reader text

    enforced by the copy-contract test over the rendered page

  • Passed

    Safety mode resolved

    Suppression classes recorded: S1, S3.

  • Passed

    Canonical metadata present

    slug and display name present

What is missing or unclearRead from sources, not yet reviewed

How this medicine reached us

Kept near the foot of the page. A historical event moves up only when it changes something about this substance today.

What the approval register records

  • 1 approved application covers products containing this substance. The earliest was NDA214783, approved 20210716 to KADMON PHARMS LLC.

    Drugs@FDA application register · NDA214783 · read 2026-08-29

  • Marketing status on the register: prescription.

    Drugs@FDA application register · NDA214783 · read 2026-08-29

  • The earliest marketing start date recorded for a listed product is 20201023.

    FDA National Drug Code directory · 50379-0028 · read 2026-08-29

What is missing or unclearRead from sources, not yet reviewed

What to learn next

Ordered by what would most change how you read this page, starting with what is easiest to misunderstand.

This order is fixed in code and does not count clicks or time on the page.

What is not here

9 questions this page could not answer

These sections were prepared and left out because there was nothing to put in them. They are listed rather than hidden, so the gaps in this record are visible.

  • What was measured, goal by goal — found nothing in the sources checked.
  • How close this is to real life — found nothing in the sources checked.
  • The path through the body — found nothing in the sources checked.
  • Felt, measured, or meaningful — found nothing in the sources checked.
  • How long anything takes — found nothing in the sources checked.
  • What it may clash with — found nothing in the sources checked.
  • Other ways to the same goal — found nothing in the sources checked.
  • Claims that go past the evidence — found nothing in the sources checked.
  • What changed on this page — found nothing in the sources checked.

The record as stored

The full record, for auditing

Everything above is built from what is below. This layer keeps the technical vocabulary, record identifiers and every stored row, so a reader who wants to check the page can.

Recorded evidence blocks (9)

On the Belumosudil label: indicated for what?


"REZUROCK is indicated for the treatment of adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy. REZUROCK is a kinase inhibitor indicated for the treatment of adult and pediatric patients 12 years and older…": indications and usage on Belumosudil's label. DailyMed label · 102e4ef4-7f84-4e34-8df1-479c24d1575d · 2026-04-07

39 registered trials of Belumosudil — at which phases?


Registered studies posting no result
26 of 39

39 registered studies of Belumosudil: 21 phase2, 13 phase1, 3 phase3, 2 early phase1, 2 phase4. CLINICALTRIALS_SNAPSHOT · 2026-09-01

14 with a PubMed record

Show the evidence
  • phase2
    21
  • phase1
    13
  • phase3
    3
  • early phase1
    2
  • phase4
    2
  • completed
    17
7 more recorded rows
  • recruiting
    10
  • not yet recruiting
    5
  • terminated
    3
  • active not recruiting
    1
  • enrolling by invitation
    1
  • unknown
    1
  • withdrawn
    1

recorded 2026-09-01 · last checked 2026-09-04

4 of Belumosudil's trials stopped: safety, sponsor decision unspecified?


safety (3) and sponsor decision unspecified (1): Belumosudil's stop wording, clustered. CLINICALTRIALS_SNAPSHOT · 2026-09-01

"The sponsor has decided to prematurely terminate the study due to the challenges encountered in recruiting adolescent participants. This decision was made without any safety concerns."; 4 of 39 registered studies

Show the evidence

Trial

  • NCT03640481
    terminated; "The sponsor has decided to prematurely terminate the study due to the challenges encountered in recruiting adolescent participants. This decision was made without any safety concerns."
  • NCT03919799
    terminated; "Sponsor decision due to slow enrollment and strategic consideration; not driven by any safety concerns."
  • NCT04680975
    terminated; "Sponsor decision due to slow enrollment and strategic consideration; not driven by any safety concerns."
  • NCT05567406
    withdrawn; "Sponsor decision."

recorded 2026-09-01 · last checked 2026-09-04

Human studies of Belumosudil used Belumosudil 200 mg tablet — over how long?


studies of Belumosudil used the recorded amount. ClinicalTrials.gov · 2026-09-01

18 recorded entries; human; tablet, IV, capsule; also "Belumosudil 200 mg tablet", "[14C]-KD025 at a dose of 100 μg in a 5 mL solution IV microdose", "[14C]-KD025 200 mg capsule"

Show the evidence

human

  • NCT03907540
    tablet; Belumosudil 200 mg tablet
  • NCT03907540
    IV; [14C]-KD025 at a dose of 100 μg in a 5 mL solution IV microdose
  • NCT03907540
    capsule; [14C]-KD025 200 mg capsule
  • NCT04735822
    Part 1: Belumosudil 40 mg/mL Sequence ABFCED
  • NCT04735822
    Part 1: Belumosudil 40 mg/mL Sequence BCADFE
  • NCT04735822
    Part 1: Belumosudil 40 mg/mL Sequence CDBEAF
12 more recorded rows
  • human NCT04735822
    Part 1: Belumosudil 40 mg/mL Sequence DECFBA
  • human NCT04735822
    Part 1: Belumosudil 40 mg/mL Sequence EFDACB
  • human NCT04735822
    Part 1: Belumosudil 40 mg/mL Sequence FAEBDC
  • human NCT04735822
    Part 2: Belumosudil 200 mg Sequence GHI
  • human NCT04735822
    Part 2: Belumosudil 200 mg Sequence HIG
  • human NCT04735822
    Part 2: Belumosudil 200 mg Sequence IGH
  • human NCT04735822
    Part 2: Belumosudil 200 mg Sequence IHG
  • human NCT04735822
    Part 2: Belumosudil 200 mg Sequence GIH
  • human NCT04735822
    Part 2: Belumosudil 200 mg Sequence HGI
  • human NCT05305989
    Belumosudil 200 mg QD
  • human NCT05305989
    Belumosudil 200 mg BID
  • human NCT05305989
    Belumosudil 400 mg QD

recorded 2026-09-01 · last checked 2026-09-04

Belumosudil's half-life is 19 hours — which schedules were studied?


19 hours, the half-life Belumosudil's label states: "Elimination The mean (%CV) elimination half-life of belumosudil was 19 hours (39%), and clearance was 9.83 L/hours (46%) in patients." DailyMed label · 102e4ef4-7f84-4e34-8df1-479c24d1575d · 2026-04-07

tmax 1.26 to 2.53 hours; bioavailability 64 %.

Show the evidence
  • half life pharmacokinetics
    19 hours; Elimination The mean (%CV) elimination half-life of belumosudil was 19 hours (39%), and clearance was 9.83 L/hours (46%) in patients.
  • tmax pharmacokinetics
    1.26 to 2.53 hours; Absorption Median T max of belumosudil at steady state was 1.26 to 2.53 hours following administration of 200 mg once daily or twice daily in patients.
  • bioavailability pharmacokinetics
    64 %; The mean (%CV) bioavailability was 64% (17%) following a single belumosudil dose in healthy subjects.
  • metabolism pharmacokinetics
    Metabolism Belumosudil is primarily metabolized by CYP3A and to a lesser extent by CYP2C8, CYP2D6, and UGT1A9, in vitro .

recorded 2026-04-07 · last checked 2026-09-04

Which running trial of Belumosudil could settle lifespan?


NCT06143891 measures Event-Free Survival (EFS), reading out 2028-09-29.

2 open trials; n 260; "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."

Show the evidence

Trial

  • NCT06143891
    "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."; n 260; "Event-Free Survival (EFS)"; 2028-09-29
  • NCT07006506
    "A Study of Belumosudil in People at Risk of Developing Graft-Versus-Host Disease After a Stem Cell Transplant"; n 46; "Change in GVHD/relapse-free survival (GRFS) at 1-year post-Hematopoietic Cell Transplantation (HCT)"; 2029-05-21

Which 6 trials of Belumosudil posted no result?


Posted no result
6 of 6 completed trials
Registrations
NCT05918627, NCT05918588, NCT05918614, NCT04735822, NCT04166942 and NCT05806567
Completion dates
oldest 2009-12-09; newest 2022-10-28
Show the evidence

Trial

  • NCT05918627
    2009-12-09
  • NCT05918588
    2014-03-06
  • NCT05918614
    2014-06-07
  • NCT04735822
    2021-09-03
  • NCT04166942
    2022-06-06
  • NCT05806567
    2022-10-28

At the median, Belumosudil's trials enrolled 36 people — anything larger?


Median enrolment
36
Largest enrolment
356
Registered trials counted
39

Belumosudil and CYP3A, BCRP and OATP1B1: shared by which compounds?


CYP3A, BCRP and OATP1B1 appear in Belumosudil's recorded interaction sentences, 8 in all. DailyMed label · 102e4ef4-7f84-4e34-8df1-479c24d1575d · 2026-04-07

CYP1A2, CYP3A, CYP3A, BCRP, OATP1B1, P-gp; 6 shared nodes; drug_interactions

Show the evidence

Interaction statement

  • drug_interactions
    Strong CYP3A Inducers : Increase REZUROCK dosage to 200 mg twice daily.
  • drug_interactions
    ( 7.1 , 2.3 ) BCRP Substrates: Avoid concomitant use with drugs that are BCRP substrates where possible.
  • drug_interactions
    ( 7.2 ) OATP1B1 Substrates: If used together, monitor patients more frequently for adverse reactions and decrease the substrates dosage(s) in accordance with the respective Prescribing Information.
  • drug_interactions
    ( 7.2 ) Certain CYP1A2, CYP3A, P-gp or UGT1A1 Substrates : Avoid concomitant use with these substrates for which minimal concentration changes may lead to serious toxicities.
  • drug_interactions
    Strong CYP3A Inducers Belumosudil is a CYP3A substrate.
  • drug_interactions
    Concomitant use of REZUROCK with strong CYP3A inducers decreases belumosudil exposure [see Clinical Pharmacology (12.3) ] , which may reduce the efficacy of REZUROCK.
2 more recorded rows
  • Interaction statement drug_interactions
    Increase the dosage of REZUROCK when used concomitantly with strong CYP3A inducers [see Dosage and Administration (2.3) ].
  • Interaction statement drug_interactions
    7.2 Effect of REZUROCK on Other Drugs BCRP and OATP1B1 Substrates Avoid concomitant use with drugs that are BCRP substrates where possible.
  • CYP1A2
    FINGOLIMOD LAURYL SULFATE, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Rasagiline, Sofpironium, Golodirsen, Tinidazole

CYP3A

  • FINGOLIMOD LAURYL SULFATE, Darunavir Propylene Glycolate, Vincristine, Naldemedine, Pemetrexed, Eravacycline, Rasburicase, Repotrectinib
  • FINGOLIMOD LAURYL SULFATE, Darunavir Propylene Glycolate, Vincristine, Naldemedine, Pemetrexed, Eravacycline, Rasburicase, Repotrectinib
  • BCRP
    TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Deoxycholic acid, Golodirsen, Naldemedine, Eravacycline, Omadacycline
  • OATP1B1
    FINGOLIMOD LAURYL SULFATE, TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Deoxycholic acid, Golodirsen, Naldemedine, Eravacycline
  • P-gp
    FINGOLIMOD LAURYL SULFATE, ERYTHROMYCIN LACTOBIONATE, Darunavir Propylene Glycolate, FOSAPREPITANT DIMEGLUMINE, TAFAMIDIS MEGLUMINE, Arimoclomol, Ceftobiprole Medocaril, Vincristine

recorded 2026-04-07 · last checked 2026-09-04

Where it is registered
Identifiers, relations and other names

The exact record

ChEMBL id
CHEMBL2005186
PubChem CID
11950170
CAS number
911417-87-3
RxCUI
2564025
InChIKey
GKHIVNAUVKXIIY-UHFFFAOYSA-N
Development code
KD-025, KD025
Also called
Rock2 inhibitor kd025, Slx-2119 free base, BELUMOSUDIL MESYLATE, slx-2119, Belumosudil mesylate [ORANGE BOOK], Belumosudil mesylate [USAN], Belumosudil mesylate [WHO-DD]
Salt form
KD025 mesylate, KD-025 MESYLATE
Trade name
Rezurock
Sources (5)

Sources

  • chembl+drugsfda+ema chembl+drugsfda+ema ·
  • CLINICALTRIALS_SNAPSHOT K1:834YJF89WO ·
  • ClinicalTrials.gov clinicaltrials.gov ·
  • DailyMed label 102e4ef4-7f84-4e34-8df1-479c24d1575d ·
  • Drugs@FDA K1:834YJF89WO ·

ChEMBL 37 — CC BY-SA 3.0 Unported · ChEMBL ATC CC BY-SA · ClinicalTrials.gov — US Government work · mixed register set; per-register licences in docs/specs/corpus-20k-sources.md · openFDA / DailyMed — US Government work

How these records are assembled · Which registers were checked

Index-quality checks
  • identity passed: no open identity hold
  • required summary fields resolved: 4 required field(s) not terminal: Why people use it, Best-supported result, Biggest unanswered question, Human evidence
  • public claims reviewed: 0 reviewed claim(s); drafts are never rendered
  • source coverage passed: 5 source rows
  • no critical contamination: no quarantine open
  • canonical metadata passed: slug and display name present
  • no raw internal fields: enforced by the copy-contract test over the rendered page

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