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Drug interactions

Methotrexate + Rolapitant

Severity: Moderate

Methotrexate and Rolapitant: 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

Rolapitant inhibits BCRP, one of the transporters involved in methotrexate efflux. Methotrexate exposure could increase, with a risk of myelosuppression, mucositis and hepatic or renal toxicity, particularly at high doses.

What this interaction means in plain words

Methotrexate and Rolapitant 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; Rolapitant belongs to Gastrointestinal Tract.

Evidence level: Low

Why it happens

Rolapitant inhibits BCRP, which may reduce methotrexate efflux and elimination.

What to do

Monitor blood counts, renal function and liver tests, and methotrexate levels with high-dose therapy. Reduce 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 Rolapitant?

MediHelp rates the interaction as moderate. Methotrexate and Rolapitant 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. Rolapitant inhibits BCRP, one of the transporters involved in methotrexate efflux. Methotrexate exposure could increase, with a risk of myelosuppression, mucositis and hepatic or renal toxicity, particularly at high doses.

How serious is the interaction between Methotrexate and Rolapitant?

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 function and liver tests, and methotrexate levels with high-dose therapy. Reduce the methotrexate dose if toxicity appears.

What other medicines interact with Rolapitant?

MediHelp also lists interactions of Rolapitant with, for example, Pimozide, Thioridazine, Atomoxetine. The full list is on the Rolapitant page.

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