Irinotecan Injection and Enasidenib: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Irinotecan Injection
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 exposure of BCRP substrate
Interaction Deep Dive
Enasidenib is an BCRP inhibitor. Coadministration of enasidenib and this drug (BCRP substrate) may increase the exposure of the BCRP 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(0 to infinity) by 244%. Decrease the dosage of the BCRP substrate as recommended and as clinically indicated1.
Why it happens (mechanism)
Inhibition of BCRP transport by enasidenib
Literature reports
1 report — 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.
Common questions
Can I take Irinotecan Injection and Enasidenib together?
Increased exposure of BCRP substrate Always confirm with your pharmacist or prescriber before making any change.
How serious is the Irinotecan Injection 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 "theoretical". Predicted from the drugs' pharmacology; not yet confirmed in people.
Questions for your pharmacist
- Does my dose of Irinotecan Injection 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 (1)
- Product Information: IDHIFA(R) oral tablets, enasidenib oral tablets. Celgene Corporation (per FDA), Summit, NJ, 2020. DailyMed
Keep reading about Irinotecan Injection
Keep reading about Enasidenib
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