Selpercatinib and Mitapivat: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Selpercatinib
Mitapivat
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 selpercatinib exposure and reduced anti-tumor activity
Interaction Deep Dive
Avoid coadministration of selpercatinib with strong or moderate CYP3A inducers because significantly reduced selpercatinib exposure may result in diminished anti-tumor activity. Coadministration of selpercatinib with multiple doses of rifAMPin (a strong CYP3A inducer) decreased selpercatinib AUC (0 to inf) by 87% and Cmax by 70%. Coadministration of multiple doses of bosentan or efavirenz (moderate CYP3A inducers) is predicted to decrease selpercatinib AUC (0 to inf) by 40% to 70% and Cmax by 34% to 57%1.
Why it happens (mechanism)
Induction of CYP3A-mediated metabolism of selpercatinib
Literature reports
2 reports — tap to read
a) In a pharmacokinetic study, coadministration of selpercatinib with multiple doses of rifAMPin (a strong CYP3A inducer) decreased selpercatinib AUC (0 to inf) by 87% and Cmax by 70% 1.
b) Simulated coadministration of multiple doses of bosentan or efavirenz (moderate CYP3A inducers) is predicted to decrease selpercatinib AUC (0 to inf) by 40% to 70% and Cmax by 34% to 57% 1.
Common questions
Can I take Selpercatinib and Mitapivat together?
Reduced selpercatinib exposure and reduced anti-tumor activity Always confirm with your pharmacist or prescriber before making any change.
How serious is the Selpercatinib and Mitapivat 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 Selpercatinib or Mitapivat 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: RETEVMO(R) oral capsules, tablets, selpercatinib oral capsules, tablets. Lilly USA LLC (per FDA), Indianapolis, IN, 2024. DailyMed
Keep reading about Selpercatinib
Keep reading about Mitapivat
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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