Relugolix and Glecaprevir: 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
Relugolix
Glecaprevir
No brand names on record
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.
These two medicines can interact. Relugolix (Orgovyx) is moved out of your body partly by a 'pump' in your gut called P-gp. Glecaprevir can block that pump. When the pump is blocked, more relugolix stays in your body, so its levels go up. In one study using a different blocker, relugolix levels rose about 3 times higher.
Higher levels can mean a greater chance of side effects like hot flashes, tiredness, or mood changes. The good news is your care team can manage this. Please don't stop or change either drug on your own. Talk with your pharmacist or doctor so they can plan the safest approach for you.
Effect: Increased relugolix exposure. Relugolix is a P-gp substrate; glecaprevir inhibits P-gp, reducing relugolix efflux and increasing its AUC/Cmax. Neither drug is a prodrug here, so the direction is straightforward: more relugolix, more potential toxicity.
- Magnitude: Reference study (erythromycin) increased relugolix AUC ~3.5-fold and Cmax ~2.9-fold.
- Evidence: Probable; severity major; onset unspecified.
- Management: Avoid coadministration if possible. If unavoidable, give relugolix first and separate dosing by at least 6 hours; monitor more frequently for adverse reactions. Relugolix may be interrupted up to 2 weeks for short P-gp inhibitor courses; if held >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 reactions 12. 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. When relugolix has been interrupted for more than 7 days, it should be restarted using a 360 mg loading dose on the first day, followed by 120 mg once daily thereafter. A drug interaction study showed that coadministering relugolix (P-gp substrate) with erythromycin (P-gp inhibitor) raised the AUC and Cmax of relugolix by 3.5-fold and 2.9-fold, respectively 1.
Why it happens (mechanism)
Inhibition of P-gp-mediated efflux transport of relugolix
How to manage this interaction
What your care team may do:
- Try to avoid using these two together when possible.
- If both are needed, take relugolix first and separate the two doses by at least 6 hours.
- Watch you more closely for relugolix side effects.
- For a short course of the interacting drug, relugolix may be paused for up to 2 weeks and restarted afterward (with a loading dose if it was held more than 7 days).
What you should do: Keep taking both exactly as prescribed and do not adjust anything yourself. Tell your pharmacist or doctor you take both so they can tailor your plan and timing.
Management is individual — confirm any change with your pharmacist or prescriber.
Literature reports
1 report — tap to read
a) In a drug interaction study, 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, respectively 1.
Common questions
Can I take Relugolix and Glecaprevir together?
Glecaprevir can raise relugolix levels by blocking a gut transporter, increasing side-effect risk, so your care team may separate the doses, monitor you closely, or briefly interrupt relugolix. Do not change anything on your own; ask your pharmacist or doctor. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Relugolix and Glecaprevir 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 Glecaprevir interaction managed?
What your care team may do: Try to avoid using these two together when possible. If both are needed, take relugolix first and separate the two doses by at least 6 hours. Watch you more closely for relugolix side effects. For a short course of the interacting drug, relugolix may be paused for up to 2 weeks and restarted afterward (with a loading dose if it was held more than 7 days). What you shoul… 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 Glecaprevir 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 Glecaprevir
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