Rosuvastatin and Belumosudil: Interaction Details
AI-assisted, pharmacist-reviewed · AI content regenerated Jul 15, 2026 · Source data updated Jul 11, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Rosuvastatin
Belumosudil
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
Here's what's going on. Belumosudil (Rezurock) slows down two of the "pumps" your body uses to move rosuvastatin (Crestor) out of your bloodstream. When those pumps are blocked, more rosuvastatin builds up than usual.
With more statin in your system, the main worry is muscle problems, like unusual muscle pain, weakness, or tenderness. In rare cases this can lead to a more serious muscle breakdown. The good news is this is very manageable. Your care team may keep your rosuvastatin dose lower while you're on both drugs and watch you more closely. Tell your pharmacist or doctor if you notice new muscle aches, weakness, or dark urine.
Mechanism: Belumosudil inhibits BCRP and OATP1B1, the transporters responsible for hepatic uptake and efflux of rosuvastatin. This reduces clearance and increases rosuvastatin systemic exposure (AUC/Cmax). Neither agent is activity-dependent on these transporters for effect, so the result is straightforward accumulation of the statin.
Direction: Increased rosuvastatin exposure, raising dose-dependent risk of myopathy and rhabdomyolysis.
- Severity: Major; evidence: probable; onset: unspecified.
- Management: Do not exceed rosuvastatin 5 mg once daily during concomitant use.
- Monitor for muscle symptoms; consider CK if symptomatic.
What happens
Increased rosuvastatin exposure and an increased risk of myopathy and rhabdomyolysis
Interaction Deep Dive
Giving rosuvastatin together with belumosudil, an inhibitor of BCRP/OATP1B1, may raise rosuvastatin exposure and heighten the likelihood of myopathy, including rhabdomyolysis. When the two are taken concurrently, rosuvastatin should be limited to no more than 5 mg once daily1.
Why it happens (mechanism)
Inhibition of BCRP-mediated efflux transport of rosuvastatin; inhibition of OATP1B1-mediated efflux transport of rosuvastatin
How to manage this interaction
This interaction can be managed. The documented guidance is clear: if these two are used together, rosuvastatin should not exceed 5 mg once daily. Your care team will individualize this.
- Keep taking both medications as prescribed unless your prescriber tells you otherwise. Do not stop or change doses on your own.
- Ask your pharmacist or doctor to confirm your rosuvastatin dose is appropriate while you're on belumosudil.
- Report any new or worsening muscle pain, tenderness, weakness, or dark-colored urine promptly.
- Your team may monitor you more closely while you take both.
Management is individual — confirm any change with your pharmacist or prescriber.
Literature reports
1 report — tap to read
a) In a drug interaction study, the coadministration of a single 10 mg dose of rosuvastatin on 2 separate days together with belumosudil 200 mg once daily for 8 days raised the rosuvastatin AUC by 4.62-fold and the Cmax by 3.59-fold, respectively 1.
Common questions
Can I take Rosuvastatin and Belumosudil together?
Belumosudil raises rosuvastatin levels and the risk of muscle injury, so rosuvastatin should be limited to 5 mg once daily when the two are taken together. Keep taking both as prescribed and report any muscle pain, weakness, or dark urine to your care team. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Rosuvastatin and Belumosudil interaction?
It is rated major. Potentially serious — often needs a change or close monitoring.
How quickly could this interaction happen?
The documented onset is "unspecified". The timing of this interaction is not well characterized.
How is the Rosuvastatin and Belumosudil interaction managed?
This interaction can be managed. The documented guidance is clear: if these two are used together, rosuvastatin should not exceed 5 mg once daily. Your care team will individualize this. Keep taking both medications as prescribed unless your prescriber tells you otherwise. Do not stop or change doses on your own. Ask your pharmacist or doctor to confirm your rosuvastatin dose is appropriate while… Management is individual — always follow your own care team's guidance.
How strong is the evidence for this interaction?
The evidence is graded "probable". Good supporting evidence, though not definitively proven.
Questions for your pharmacist
- Does my dose of Rosuvastatin or Belumosudil need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (1)
- Product Information: CRESTOR® oral tablets, rosuvastatin calcium oral tablets. AstraZeneca Pharmaceuticals LP, Wilmington, DE, 2026. DailyMed
Keep reading about Rosuvastatin
Keep reading about Belumosudil
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