Drug interactions
Regorafenib + Rifampin
Severity: Major
Regorafenib and Rifampin: major interaction.
Last updated
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
Rifampin strongly induces CYP3A4 and lowers regorafenib concentrations, which may compromise cancer treatment. Exposure to the M-5 metabolite may rise. Labeling recommends avoiding strong inducers.
What this interaction means in plain words
Regorafenib and Rifampin 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.
Why it happens
Rifampin induces CYP3A4 (and UGT1A9), increasing regorafenib clearance.
What to do
Avoid concomitant use and select an alternative antimicrobial where feasible. If unavoidable, monitor for loss of efficacy and for toxicity.
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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Other interactions of Regorafenib
Frequently asked questions
Can I take Regorafenib with Rifampin?
MediHelp rates the interaction as major. Regorafenib and Rifampin 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. Rifampin strongly induces CYP3A4 and lowers regorafenib concentrations, which may compromise cancer treatment. Exposure to the M-5 metabolite may rise. Labeling recommends avoiding strong inducers.
How serious is the interaction between Regorafenib and Rifampin?
MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Avoid concomitant use and select an alternative antimicrobial where feasible. If unavoidable, monitor for loss of efficacy and for toxicity.
What other medicines interact with Regorafenib?
MediHelp also lists interactions of Regorafenib with, for example, Apalutamide, Atazanavir, Carbamazepine. The full list is on the Regorafenib page.
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