Methotrexate Injection and Voclosporin: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Methotrexate Injection
Voclosporin
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 OATP1B1 substrate exposure
Interaction Deep Dive
Coadministration of voclosporin (a OATP1B1 inhibitor) and an OATP1B1 substrate may increase the exposure of the substrate, which may increase the incidence and severity of adverse reactions. Monitor for adverse events and reduce dosage of the substrate as needed. Coadministration of voclosporin (OATP1B1 inhibitor) 23.7 mg twice daily and simvastatin acid (OATP1B1 substrate) increased the simvastatin acid AUC by 1.84-fold and Cmax by 3.1-fold. Coadministration of voclosporin with simvastatin increased the Cmax of parent drug simvastatin by 1.6-fold but did not change AUC of simvastatin1.
Why it happens (mechanism)
Inhibition of OATP1B1-mediated efflux transport by voclosporin
Literature reports
1 report — tap to read
a) Coadministration of voclosporin (OATP1B1 inhibitor) 23.7 mg twice daily and simvastatin acid (OATP1B1 substrate) increased the simvastatin acid AUC by 1.84-fold and Cmax by 3.1-fold. Coadministration of voclosporin with simvastatin increased the Cmax of parent drug simvastatin by 1.6-fold but did not change AUC of simvastatin 1.
Common questions
Can I take Methotrexate Injection and Voclosporin together?
Increased OATP1B1 substrate exposure Always confirm with your pharmacist or prescriber before making any change.
How serious is the Methotrexate Injection and Voclosporin 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 "probable". Good supporting evidence, though not definitively proven.
Questions for your pharmacist
- Does my dose of Methotrexate Injection or Voclosporin 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 (1)
- Product Information: LUPKYNIS(TM) oral capsules, voclosporin oral capsules. Aurinia Pharma US Inc (per FDA), Rockville, MD, 2024. DailyMed
Keep reading about Methotrexate Injection
Keep reading about Voclosporin
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