Repotrectinib and Cyclosporine Injection: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Cyclosporine Injection
Repotrectinib
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 repotrectinib exposure, an increased risk of repotrectinib-related adverse effects, reduced cycloSPORINE exposure and reduced efficacy of cycloSPORINE
Interaction Deep Dive
Avoid concomitant use of repotrectinib with cycloSPORINE (P-gp inhibitor, moderate CYP3A inhibitor and a CYP3A4 substrate with NTI). Concomitant use of repotrectinib with a dual P-gp and CYP3A inhibitor may increase repotrectinib exposure, which may increase the incidence and severity of adverse reactions of repotrectinib. Also, concomitant use of repotrectinib decreases the concentration of CYP3A4 substrates, where minimal concentration changes can cause reduced efficacy. If concomitant use is unavoidable, discontinue CYP3A inhibitors for 3 to 5 elimination half-lives of the CYP3A inhibitor prior to initiating repotrectinib and increase the CYP3A4 substrate dosage as required1.
Why it happens (mechanism)
Inhibition of CYP3A-mediated metabolism of repotrectinib; inhibition of P-gp-mediated efflux transport of repotrectinib; induction of CYP3A4-substrate metabolism by repotrectinib
Literature reports
2 reports — tap to read
a) In the drug interaction studies, repotrectinib AUC (0 to inf) increased by 5.9-fold and Cmax by 1.7-fold following concomitant use with itraconazole (a strong CYP3A and P-gp inhibitor) 1.
b) In the drug interaction studies, midazolam (CYP3A4 substrate) AUC (0 to inf) decreased by 69% and Cmax by 48% following concomitant use in subjects who were previously administered 160 mg repotrectinib once daily for 14 days followed by 160 mg twice daily for 7 days 1.
Common questions
Can I take Repotrectinib and Cyclosporine Injection together?
Increased repotrectinib exposure, an increased risk of repotrectinib-related adverse effects, reduced cycloSPORINE exposure and reduced efficacy of cycloSPORINE Always confirm with your pharmacist or prescriber before making any change.
How serious is the Repotrectinib and Cyclosporine Injection 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 Repotrectinib or Cyclosporine 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 a safer alternative to one of these medications for me?
References (1)
- Product Information: AUGTYRO(TM) oral capsules, repotrectinib oral capsules. Bristol-Myers Squibb Company (per FDA), Princeton, NJ, 2023. DailyMed
Keep reading about Cyclosporine Injection
Keep reading about Repotrectinib
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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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