Drug interactions
Irinotecan + Regorafenib
Severity: Major
Irinotecan and Regorafenib: major interaction.
Last updated Sources: UK SmPC
For healthcare professionals — reference only. This page is a brief summary, not medical advice and not a substitute for official labeling or clinical judgement. Always verify before prescribing or dispensing.
Summary
Regorafenib inhibits UGT1A1 and BCRP, both involved in the disposition of irinotecan and its active metabolite SN-38. Exposure to SN-38 may increase, raising the risk of neutropenia and diarrhea.
What this interaction means in plain words
Irinotecan and Regorafenib can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for.
Irinotecan belongs to Oncology; Regorafenib belongs to Oncology.
Why it happens
Regorafenib inhibits UGT1A1-mediated glucuronidation and BCRP efflux of SN-38 and irinotecan.
What to do
Monitor blood counts and diarrhea closely and consider irinotecan dose reduction if toxicity emerges. Manage diarrhea promptly.
What to ask your pharmacist
- Does the benefit of taking both outweigh the risk in my case?
- Do I need any blood test, ECG or other check while on both?
- What early warning signs should I watch for, and what should I do if they appear?
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References
- CAMPTO 20 mg/ml, concentrate for solution for infusion (100mg & 300mg presentation) - SmPC sections 4.3/4.5 (names the partner; "APC of 87% and in an increase in the AUC of SN-38 of 109% in comparison to irinotecan given alone. UGT1A1 inhibitors: (e.g. atazanavir, ketoconazole, regorafeni") — electronic medicines compendium (UK SmPC)
Other interactions of Irinotecan
- Clozapine + Irinotecan Contraindicated
- Irinotecan + Sacituzumab govitecan Contraindicated
- Adenovirus types 4 and 7 live + Irinotecan Major
- Apalutamide + Irinotecan Major
- Atazanavir + Irinotecan Major
- Carbamazepine + Irinotecan Major
Other interactions of Regorafenib
Frequently asked questions
Can I take Irinotecan with Regorafenib?
MediHelp rates the interaction as major. Irinotecan and Regorafenib can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for. Regorafenib inhibits UGT1A1 and BCRP, both involved in the disposition of irinotecan and its active metabolite SN-38. Exposure to SN-38 may increase, raising the risk of neutropenia and diarrhea.
How serious is the interaction between Irinotecan and Regorafenib?
MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Monitor blood counts and diarrhea closely and consider irinotecan dose reduction if toxicity emerges. Manage diarrhea promptly.
What other medicines interact with Irinotecan?
MediHelp also lists interactions of Irinotecan with, for example, Clozapine, Sacituzumab govitecan, Adenovirus types 4 and 7 live. The full list is on the Irinotecan page.
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