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Drug interactions

Methotrexate + Regorafenib

Severity: Moderate

Methotrexate and Regorafenib: moderate 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

Regorafenib may inhibit BCRP, a transporter involved in methotrexate efflux, potentially increasing methotrexate exposure and toxicity such as myelosuppression and mucositis. Clinical data are limited.

What this interaction means in plain words

Methotrexate and Regorafenib can affect each other. The combination is often manageable, but it may need a change of dose, a change of timing, or extra checks while both are taken.

Methotrexate belongs to Oncology; Regorafenib belongs to Oncology.

Evidence level: Low

Why it happens

Inhibition of BCRP (ABCG2)-mediated efflux of methotrexate by regorafenib.

What to do

Monitor blood counts, renal and liver function and signs of methotrexate toxicity; consider lowering the methotrexate dose if toxicity appears.

What to ask your pharmacist

  • Should I take them at different times of day?
  • Does the dose of either medicine need to change?
  • Is there anything I should avoid, such as alcohol or certain foods, while on both?

Bring a full list of your medicines, including over-the-counter products, supplements and herbal remedies, to every pharmacy visit.

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Frequently asked questions

Can I take Methotrexate with Regorafenib?

MediHelp rates the interaction as moderate. Methotrexate and Regorafenib can affect each other. The combination is often manageable, but it may need a change of dose, a change of timing, or extra checks while both are taken. Regorafenib may inhibit BCRP, a transporter involved in methotrexate efflux, potentially increasing methotrexate exposure and toxicity such as myelosuppression and mucositis. Clinical data are limited.

How serious is the interaction between Methotrexate and Regorafenib?

MediHelp rates it moderate, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Monitor blood counts, renal and liver function and signs of methotrexate toxicity; consider lowering the methotrexate dose if toxicity appears.

What other medicines interact with Methotrexate?

MediHelp also lists interactions of Methotrexate with, for example, Acitretin, Adenovirus types 4 and 7 live, Influenza virus vaccine quadrivalent intranasal. The full list is on the Methotrexate page.

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