Relugolix and Elagolix: Interaction Details
AI-assisted, pharmacist-reviewed · AI content regenerated Jul 11, 2026 · Source data updated Jul 2, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Elagolix
Relugolix
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.
If you take relugolix (Orgovyx) and elagolix (Orilissa) together, the elagolix can slow down a 'pump' in your gut that normally pushes relugolix back out of your body. When that pump is blocked, more relugolix stays in your system than intended. In one study of a similar blocker, relugolix levels rose about 3 times higher.
Higher levels can mean a greater chance of relugolix side effects. The good news is your care team can manage this by spacing the doses out, watching you more closely, or adjusting your plan. Please don't stop or change either medicine on your own, just check with your pharmacist or doctor.
Effect: Increased relugolix exposure. Elagolix inhibits P-gp-mediated efflux of relugolix (a P-gp substrate), raising systemic exposure and adverse-reaction risk. Neither drug is a prodrug, so this is a true increase in active drug.
Magnitude: With erythromycin (P-gp inhibitor), relugolix AUC rose 3.5-fold and Cmax 2.9-fold. Evidence: probable. Severity: major.
- Avoid concomitant use where possible.
- If unavoidable: give relugolix (or relugolix/estradiol/norethindrone) first, separate by at least 6 hours, monitor more frequently.
- Relugolix may be interrupted up to 2 weeks for a short P-gp inhibitor course; if held greater than 7 days, restart with 360 mg loading dose, then 120 mg daily.
What happens
Increased relugolix exposure
Interaction Deep Dive
Do not use relugolix (a P-gp substrate) together with P-gp inhibitors, since doing so can raise relugolix exposure and thereby heighten the likelihood of adverse reactions linked to relugolix. When coadministration cannot be avoided, give relugolix or relugolix/estradiol/norethindrone acetate first, keep the doses at least 6 hours apart, and increase the frequency of monitoring for adverse reactions12. Relugolix therapy may be paused for as long as 2 weeks to accommodate a brief course of certain P-gp inhibitors, resuming relugolix once the P-gp inhibitor has been stopped. Should relugolix be interrupted for more than 7 days, restart it using a loading dose of 360 mg on the first day, followed by 120 mg once daily. In a drug interaction study, giving relugolix (P-gp substrate) alongside erythromycin (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 combination is generally best avoided, but your care team has clear ways to handle it if you need both.
- Keep taking both as prescribed unless your prescriber tells you otherwise.
- Your team may have you take relugolix first and separate the two doses by at least 6 hours.
- They may monitor you more closely for relugolix side effects.
- Sometimes relugolix is paused during a short course of the other drug and restarted afterward, with the dose individualized by your team.
Ask your pharmacist or doctor how to best time these medicines and what side effects to watch for.
Management is individual — confirm any change with your pharmacist or prescriber.
Literature reports
1 report — tap to read
a) In a study of drug interactions, giving relugolix (a P-gp substrate) together with erythromycin (a P-gp inhibitor) raised relugolix's AUC by 3.5-fold and its Cmax by 2.9-fold 1.
Common questions
Can I take Relugolix and Elagolix together?
Elagolix can significantly raise relugolix levels by blocking its efflux pump, increasing side-effect risk. Avoid using them together if possible, and let your care team space the doses and monitor you if both are needed. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Relugolix and Elagolix 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 Relugolix and Elagolix interaction managed?
This combination is generally best avoided, but your care team has clear ways to handle it if you need both. Keep taking both as prescribed unless your prescriber tells you otherwise. Your team may have you take relugolix first and separate the two doses by at least 6 hours. They may monitor you more closely for relugolix side effects. Sometimes relugolix is paused during a short course of the oth… 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 Relugolix or Elagolix 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 Elagolix
Keep reading about Relugolix
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