Alpelisib and Mitotane: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Jul 11, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Mitotane
Alpelisib
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
Reduced alpelisib exposure and reduced efficacy of alpelisib
Interaction Deep Dive
Avoid coadministration of alpelisib (a CYP3A4 substrate) with strong CYP3A4 inducers, as concomitant use of these agents may reduce alpelisib exposure, which may reduce alpelisib efficacy. Coadministration of repeat doses of rifAMPin (a strong CYP3A4 inducer) with a single 300 mg dose of alpelisib decreased alpelisib Cmax by 38% and AUC by 57%, respectively. Coadministration of rifAMPin with repeat doses of 300 mg alpelisib decreased alpelisib Cmax by 59% and AUC by 74%, respectively. Consider an alternative concomitant drug with no or minimal potential to induce CYP3A412.
Why it happens (mechanism)
Induction of CYP3A4-mediated metabolism of alpelisib
Literature reports
1 report — tap to read
a) Coadministration of repeat doses of rifAMPin (a strong CYP3A4 inducer) with a single 300 mg dose of alpelisib decreased alpelisib Cmax by 38% and AUC by 57%, respectively. Coadministration of rifAMPin with repeat doses of 300 mg alpelisib decreased alpelisib Cmax by 59% and AUC by 74%, respectively 12.
Common questions
Can I take Alpelisib and Mitotane together?
Reduced alpelisib exposure and reduced efficacy of alpelisib Always confirm with your pharmacist or prescriber before making any change.
How serious is the Alpelisib and Mitotane 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 Alpelisib or Mitotane 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)
- Product Information: VIJOICE(R) oral tablets, oral granules, alpelisib oral tablets, oral granules. Novartis Pharmaceuticals Corporation (per FDA), East Hanover, NJ, 2025. DailyMed
- Product Information: PIQRAY(R) oral tablets, alpelisib oral tablets. Novartis Pharmaceuticals Corporation (per FDA), East Hanover, NJ, 2024. DailyMed
Keep reading about Mitotane
Keep reading about Alpelisib
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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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