Axitinib and Enasidenib: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Axitinib
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
Altered (increased/reduced) axitinib exposure and an increased risk of axitinib-related adverse effects or reduced efficacy of axitinib
Interaction Deep Dive
Avoid coadministration of enasidenib and axitinib. Enasidenib is an OATP1B1 inhibitor and a CYP3A inducer. Coadministration of enasidenib and axitinib (OATP1B1 and CYP3A substrate with NTI) may either increase the exposure of axitinib or decrease the exposure of axitinib, for which minimal concentration changes may lead to serious toxicities or may lead to reduced efficacy of axitinib. If coadministration cannot be avoided, modify the dosage of axitinib as recommended and as clinically indicated1.
Why it happens (mechanism)
Inhibition of OATP1B1-efflux transport by enasidenib; induction of CYP3A-substrate metabolism 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) In the drug interaction studies, midazolam (a sensitive CYP3A substrate) AUC (0 to inf) and Cmax decreased by 43% and 23%, respectively, following concomitant use of multiple doses of enasidenib 100 mg with a single intravenous dose of midazolam 0.03 mg/kg. The decrease in midazolam exposure following oral administration of midazolam is expected to be larger than that following intravenous administration of midazolam. This is due to induction of CYP3A4 first pass metabolism by enasidenib and the reduced bioavailability of the midazolam oral formulation compared to the midazolam intravenous formulation 1.
Common questions
Can I take Axitinib and Enasidenib together?
Altered (increased/reduced) axitinib exposure and an increased risk of axitinib-related adverse effects or reduced efficacy of axitinib Always confirm with your pharmacist or prescriber before making any change.
How serious is the Axitinib 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 Axitinib 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. Bristol-Myers Squibb (per FDA), Princeton, NJ, 2023. DailyMed
Keep reading about Axitinib
Keep reading about Enasidenib
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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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