Rosuvastatin and Enasidenib: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Rosuvastatin
Enasidenib
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.
What happens
Increased rosuvastatin exposure and an increased risk of myopathy and rhabdomyolysis
Interaction Deep Dive
Enasidenib is an OATP1B1 and BCRP inhibitor. Coadministration of enasidenib and rosuvastatin (a OATP1B1 and BCRP substrate) may increase the exposure of the substrate, which may increase the incidence and severity of adverse reactions. Coadministration of rosuvastatin (OATP1B1, OATP1B3, and BCRP substrate) with enasidenib increased rosuvastatin Cmax by 366% and AUC by 244%. Decrease the dosage of the substrate as recommended and as clinically indicated1. Enasidenib increased rosuvastatin exposure more than 2.4-fold. The risk of myopathy and rhabdomyolysis is increased with concomitant use of rosuvastatin and enasidenib. In patients taking enasidenib, do not exceed a dose of rosuvastatin 10 mg once daily 2.
Why it happens (mechanism)
Inhibition of OATP1B1-mediated efflux transport by enasidenib; inhibition of BCRP-mediated efflux transport by enasidenib
Literature reports
2 reports — tap to read
a) Coadministration of rosuvastatin 10 mg (OATP1B1, OATP1B3, and BCRP substrate) after multiple doses of enasidenib 100 mg (OATP1B1, OATP1B3, and BCRP inhibitor) increased rosuvastatin Cmax by 366% and AUC(0 to infinity) by 244% 1.
b) Drug interaction studies, concomitant administration of rosuvastatin 10 mg single dose with enasidenib 100 mg once daily for 28 days increased the rosuvastatin AUC and Cmax. The mean ratio of rosuvastatin with or with out enasidenib for AUC and Cmax were 2.44 and 3.66 respectively 2.
Common questions
Can I take Rosuvastatin and Enasidenib 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 Rosuvastatin and Enasidenib 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 Rosuvastatin or Enasidenib 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 (2)
Keep reading about Rosuvastatin
Keep reading about Enasidenib
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:
major · moderate · minor — check everything you take with our drug–supplement interaction checker.
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