Tafamidis and Methotrexate Injection: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Methotrexate Injection
Tafamidis
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
What happens
Increased BCRP substrate exposure and an increased risk of the substrate-related toxicities
Interaction Deep Dive
Coadministration of tafamidis (a BCRP inhibitor) and a BCRP substrate may result in increased exposure of the BCRP substrate and risk of substrate-related toxicities. Coadministration of tafamidis 61 mg daily with rosuvastatin (a BCRP substrate) resulted in an increase in rosuvastatin AUC(infinity) by 97% and Cmax by 86%. If coadministered, monitor patients for signs of substrate-related toxicities and adjust the dosage of the substrate as needed1.
Why it happens (mechanism)
Inhibition of BCRP-mediated substrate metabolism by tafamidis
Literature reports
2 reports — tap to read
a) During drug interaction studies, administration of a single dose of rosuvastatin 10 mg to patients receiving tafamidis (61 mg once daily) resulted in 1.97-fold increase in the AUC and 1.86-fold increase in the Cmax of rosuvastatin 2.
b) In a drug interaction study in healthy subjects, coadministration of tafamidis 61 mg daily with rosuvastatin (a BCRP substrate) resulted in an increase in rosuvastatin AUC(infinity) by 96.75% and Cmax by 85.59% 1.
Common questions
Can I take Tafamidis and Methotrexate Injection together?
Increased BCRP substrate exposure and an increased risk of the substrate-related toxicities Always confirm with your pharmacist or prescriber before making any change.
How serious is the Tafamidis and Methotrexate Injection interaction?
It is rated major. Potentially serious — often needs a change or close monitoring.
How quickly could this interaction happen?
The documented onset is "unspecified". The timing of this interaction is not well characterized.
How strong is the evidence for this interaction?
The evidence is graded "theoretical". Predicted from the drugs' pharmacology; not yet confirmed in people.
Questions for your pharmacist
- Does my dose of Tafamidis or Methotrexate Injection need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (2)
Keep reading about Methotrexate Injection
Keep reading about Tafamidis
These medications also interact with supplements
Prescription drugs aren't the whole picture — herbal and dietary supplements can interact with them too. From the evidence-graded Natural Medicines database:
major · moderate · minor — check everything you take with our drug–supplement interaction checker.
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