Rolapitant and Methotrexate Interaction

Drug interaction information between Rolapitant and Methotrexate.

Rolapitant and Methotrexate have a documented minor interaction in FDA labeling.

FDA drug labeling documents a minor-severity interaction between Rolapitant and Methotrexate. This page displays the available source-record category and label text. The category is not an individual risk estimate or medication-combination direction.

Drug A

Rolapitant

NK1 Receptor Antagonist (Antiemetic)

Drug B

Methotrexate

Disease-Modifying Antirheumatic Drug (DMARD)

How They Interact

Rolapitant blocks a protein that removes methotrexate from your system, which can cause the drug to build up to unsafe levels.

FDA Label Information

BCRP Substrates with a Narrow Therapeutic Index (e.g., methotrexate, topotecan, or irinotecan) Clinical Impact: Increased plasma concentrations of BCRP substrates (e.g., methotrexate, topotecan, or irinotecan) may result in potential adverse reactions [see Clinical Pharmacology (12.3) ].

Methotrexate Also Interacts With

View all Methotrexate interactions →

Frequently Asked Questions

What SPL severity band is on file for Rolapitant + Methotrexate?

Compiled FDA labeling labels this pair minor. That is a source-record field, not an individual medication-combination decision.

Which drug in this pair has the larger labeled-interaction portfolio?

Methotrexate has 38 labeled pairs on file vs Rolapitant's 9. In the minor band specifically: Rolapitant has 6 (also Rosuvastatin, Warfarin, Digoxin, Dextromethorphan); Methotrexate has 26 (also Aspirin, Folic Acid, Probenecid, Phenytoin).

What mechanism field is on file for Rolapitant and Methotrexate?

Rolapitant blocks a protein that removes methotrexate from your system, which can cause the drug to build up to unsafe levels.

Rolapitant carries more major-labeled pairs than Methotrexate

SPL source-record counts only. This page's band is minor · classes on file: Rolapitant (NK1 Receptor Antagonist (Antiemetic)); Methotrexate (Disease-Modifying Antirheumatic Drug (DMARD)).

Rolapitant has 2 major-labeled pairs vs Methotrexate's 0. This page itself is in the minor band, not the major band.

Rolapitant

2 major · 1 moderate · 6 minor · 9 total

Methotrexate

0 major · 12 moderate · 26 minor · 38 total

Sources: FDA Drug Labels (SPL) via openFDA (2026). This is for informational purposes only and is not medical advice. This registry does not provide individual medication-combination directions.