Irinotecan Injection and Darolutamide: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Irinotecan Injection
Darolutamide
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 plasma concentrations of BCRP substrates
Interaction Deep Dive
Concomitant use of darolutamide (a BCRP inhibitor) and a BCRP substrate may lead to increased exposure and adverse reactions of the BCRP substrate. Concurrent use of darolutamide with rosuvastatin (BCRP, OATP1B1 and OATP1B3 substrate) significantly increased rosuvastatin exposure by 5-fold. Avoid concomitant use of darolutamide and a BCRP transporter substrate when possible. If coadministration is required, increase monitoring for substrate toxicity and consider substrate dosage reduction1.
Why it happens (mechanism)
Inhibition of BCRP-mediated transport efflux by darolutamide
Literature reports
1 report — tap to read
a) During a pharmacokinetic study, coadministration of darolutamide with rosuvastatin (BCRP, OATP1B1 and OATP1B3 substrate) increased rosuvastatin AUC and Cmax by approximately 5-fold 1.
Common questions
Can I take Irinotecan Injection and Darolutamide together?
Increased plasma concentrations of BCRP substrates Always confirm with your pharmacist or prescriber before making any change.
How serious is the Irinotecan Injection and Darolutamide 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 Irinotecan Injection or Darolutamide 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: NUBEQA(R) oral tablets, darolutamide oral tablets. Bayer HealthCare Pharmaceuticals Inc (per FDA), Whippany, NJ, 2021. DailyMed
Keep reading about Irinotecan Injection
Keep reading about Darolutamide
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