Crizotinib and Midazolam Injection: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Crizotinib
Midazolam Injection
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 midazolam exposure
Interaction Deep Dive
The concomitant use of crizotinib (a moderate CYP3A inhibitor) with midazolam (a CYP3A substrate) increases midazolam plasma concentrations. In one study, the concomitant use of crizotinib with midazolam increased midazolam AUC by 3.7-fold compared with midazolam exposure alone. Dose reduction of midazolam may be required when coadministered with crizotinib1.
Why it happens (mechanism)
Inhibition of CYP3A-mediated midazolam metabolism by crizotinib
Literature reports
1 report — tap to read
a) The coadministration of crizotinib 250 mg twice daily for 28 days with midazolam (a CYP3A substrate) resulted in a geometric mean increase of oral midazolam AUC that was 3.7-fold compared with midazolam exposure alone. This suggests that crizotinib is a moderate inhibitor of CYP3A 1.
Common questions
Can I take Crizotinib and Midazolam Injection together?
Increased midazolam exposure Always confirm with your pharmacist or prescriber before making any change.
How serious is the Crizotinib and Midazolam Injection interaction?
It is rated moderate. Can be significant — usually manageable with 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 Crizotinib or Midazolam Injection 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 anything you'd monitor while I'm on both?
References (1)
- Product Information: XALKORI(R) oral pellets, oral capsules, crizotinib oral pellets, oral capsules. Pfizer Labs (per FDA), New York, NY, 2023. DailyMed
Keep reading about Crizotinib
Keep reading about Midazolam Injection
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.
Check another combination
Our instant two-drug interaction checker is almost here.
Still have questions about this combination?
Every question gets a real answer from a licensed pharmacist — free, and usually within a day.
Ask the pharmacist