Drug Interaction Report

Leflunomide and Rosuvastatin: Interaction Details

A pharmacist-reviewed analysis of the Leflunomide and Rosuvastatin interaction: the documented clinical effects, severity rating, onset, mechanism, and management considerations, with cited references throughout.

AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature

Leflunomide

Arava Arava®
+

Rosuvastatin

Crestor Crestor® Ezallor Ezallor®
Dr. Brian Staiger, PharmD, BCPS
Medically reviewed by
Dr. Brian Staiger, PharmD, BCPS
Updated Aug 8, 2026
Editorial policy · Data sources
LinkedIn
Interaction severity
Major
Potentially serious — often needs a change or close monitoring.
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.

Of 58 documented Leflunomide interactions, 52 are rated major — including this one.
Worried about symptoms right now? Contact your pharmacist or prescriber, or call Poison Control at 1-800-222-1222 (US). Call 911 for an emergency.
Onset
unspecified
Evidence
probable
Severity
Major

What happens

Increased rosuvastatin exposure and an increased risk of myopathy and rhabdomyolysis

Interaction Deep Dive

Concomitant use of rosuvastatin (a BCRP and OAT substrate) and teriflunomide (BCRP and OAT inhibitor; the active metabolite of leflunomide1), may increase rosuvastatin exposure 23 and may increase the risk of myopathy and rhabdomyolysis 3. When multiple doses of teriflunomide were coadministered with rosuvastatin, there was an mean 2.51-fold increase in rosuvastatin AUC and 2.65-fold increase in Cmax 23. If coadministered, do not exceed rosuvastatin 10 mg orally once daily and monitor closely for rosuvastatin associated adverse events 23.

Why it happens (mechanism)

Inhibition of BCRP-mediated efflux transport of rosuvastatin; inhibition of OAT1B1-mediated efflux transport of rosuvastatin; inhibition of OAT1B3-mediated efflux transport of rosuvastatin

Literature reports

1 report — tap to read

a) When multiple doses of teriflunomide were coadministered with rosuvastatin, there was an mean 2.51-fold increase in rosuvastatin AUC and 2.65-fold increase in Cmax 23.

Common questions

Can I take Leflunomide and Rosuvastatin together?

Increased rosuvastatin exposure and an increased risk of myopathy and rhabdomyolysis Always confirm with your pharmacist or prescriber before making any change.

How serious is the Leflunomide and Rosuvastatin 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 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 Leflunomide or Rosuvastatin 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 (3)

  1. Product Information: ARAVA(R) oral tablets, leflunomide oral tablets. Sanofi-Aventis U.S. LLC (per FDA), Bridgewater, NJ, 2016. DailyMed
  2. Product Information: AUBAGIO(R) oral tablets, teriflunomide oral tablets. Genzyme Corporation (per FDA), Cambridge, MA, 2014. DailyMed
  3. Product Information: CRESTOR(R) oral tablets, rosuvastatin calcium oral tablets. AstraZeneca Pharmaceuticals LP (per FDA), Wilmington, DE, 2023. DailyMed
Was this write-up helpful?
Leflunomide

Keep reading about Leflunomide

All Leflunomide interactions (58) Leflunomide drug information
Also serious with: Teriflunomide Letermovir Injection Acyclovir Methotrexate Injection
Rosuvastatin

Keep reading about Rosuvastatin

All Rosuvastatin interactions (24) Rosuvastatin drug information
Also serious with: Cyclosporine Injection Asciminib Eluxadoline Niacin
Beyond drug–drug

These medications also interact with supplements

Prescription drugs aren't the whole picture — herbal and dietary supplements can interact with them too. From the evidence-graded Natural Medicines database:

Leflunomide + Activated Charcoal Beer Siberian Cocklebur Wine Ashwagandha Black Cohosh Boldo Buchu + 51 more
Rosuvastatin + Activated Charcoal Beer Grapefruit Siberian Cocklebur Wine Ashwagandha Black Cohosh Black Tea + 55 more

major · moderate · minor — check everything you take with our drug–supplement interaction checker.

Check another combination

Our instant two-drug interaction checker is almost here.

Coming soon

The instant two-drug checker is on its way.

In the meantime, browse the directory below to look up any drug and see its documented interactions.

Still have questions about this combination?

Every question gets a real answer from a licensed pharmacist — free, and usually within a day.

Ask the pharmacist
This information is for education, not a substitute for professional medical advice. Do not start, stop, or change any medication without talking to your pharmacist or prescriber.