Abrocitinib and Relugolix: Interaction Details
AI-assisted, pharmacist-reviewed · AI content regenerated Jul 11, 2026 · Source data updated Jul 10, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Relugolix
Abrocitinib
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.
You've been prescribed relugolix (Orgovyx) and abrocitinib (Cibinqo). Here's the plain-English version: your body normally pumps some relugolix back out using a transporter called P-gp. Abrocitinib can slow that pump down, so more relugolix stays in your system. Higher levels mean a higher chance of relugolix side effects, like hot flashes, tiredness, or joint discomfort.
This is considered a serious interaction, but it's very manageable. Your care team can space the doses out, watch you a little more closely, or adjust your plan. Please don't stop or change either medicine on your own, just talk with your pharmacist or doctor first.
Effect: Increased relugolix exposure. Relugolix is a P-gp substrate; abrocitinib inhibits P-gp-mediated efflux, reducing relugolix clearance and raising AUC/Cmax. Neither is a prodrug here, so the direction is increased relugolix effect and toxicity risk.
Magnitude: As a reference, erythromycin (a P-gp inhibitor) raised relugolix AUC 3.5-fold and Cmax 2.9-fold. Evidence: probable. Onset: unspecified. Rated major.
- Avoid concomitant use where possible.
- If unavoidable, give relugolix first and separate by at least 6 hours.
- Monitor for relugolix-related adverse reactions more frequently.
- Relugolix may be interrupted up to 2 weeks for short P-gp inhibitor courses; if held greater than 7 days, restart with 360 mg loading dose then 120 mg daily.
What happens
Increased relugolix exposure
Interaction Deep Dive
Concurrent administration of relugolix (a P-gp substrate) with P-gp inhibitors should be avoided, since this can raise relugolix exposure and thereby heighten the likelihood of relugolix-related adverse reactions. When coadministration cannot be avoided, give relugolix or relugolix/estradiol/norethindrone acetate first, allow a gap of at least 6 hours between doses, and increase the frequency of monitoring for adverse reactions12. For a brief course of certain P-gp inhibitors, relugolix therapy may be paused for as long as 2 weeks. Once the P-gp inhibitor has been stopped, relugolix can be resumed. Should relugolix be interrupted for more than 7 days, reinitiate it using a 360 mg loading dose on the first day, then continue at 120 mg once daily. A drug interaction study found that giving relugolix (a P-gp substrate) together with erythromycin (a P-gp inhibitor) raised the AUC and Cmax of relugolix by 3.5-fold and 2.9-fold, respectively1.
Why it happens (mechanism)
Inhibition of P-gp-mediated efflux transport of relugolix
How to manage this interaction
This interaction is manageable with a few practical steps your care team may use:
- Keep taking both as prescribed unless your prescriber tells you otherwise.
- Your team may avoid combining them when possible, or arrange dose timing so relugolix is taken first with doses separated by at least 6 hours.
- They may monitor you more closely for relugolix side effects.
- In some cases relugolix may be paused for a short course of the other drug and restarted afterward, with the dose individualized by your team.
Ask your pharmacist or doctor how they'd like you to space the doses and what side effects to report.
Management is individual — confirm any change with your pharmacist or prescriber.
Literature reports
1 report — tap to read
a) In a study evaluating drug interactions, giving relugolix (a P-gp substrate) together with erythromycin (a P-gp inhibitor) raised the AUC of relugolix by 3.5-fold and its Cmax by 2.9-fold 1.
Common questions
Can I take Abrocitinib and Relugolix together?
Abrocitinib can raise relugolix levels and side effect risk by blocking a transporter that clears it; your care team can manage this by spacing doses (relugolix first, at least 6 hours apart), monitoring you more closely, or adjusting your plan. Do not change either medicine on your own. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Abrocitinib and Relugolix 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 is the Abrocitinib and Relugolix interaction managed?
This interaction is manageable with a few practical steps your care team may use: Keep taking both as prescribed unless your prescriber tells you otherwise. Your team may avoid combining them when possible, or arrange dose timing so relugolix is taken first with doses separated by at least 6 hours. They may monitor you more closely for relugolix side effects. In some cases relugolix may be paused… Management is individual — always follow your own care team's guidance.
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 Abrocitinib or Relugolix 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)
- Product Information: ORGOVYX oral tablets, relugolix oral tablets. Sumitomo Pharma America, Inc (per FDA), Marlborough, MA, 2025. DailyMed
- Product Information: MYFEMBREE(R) oral tablets, relugolix, estradiol, norethindrone acetate oral tablets. Myovant Sciences Inc (per FDA), Brisbane, CA, 2021. DailyMed
Keep reading about Relugolix
Keep reading about Abrocitinib
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