Boceprevir and Relugolix: 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
Boceprevir
No brand names on recordRelugolix
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.
Let's talk about taking relugolix (Orgovyx) together with boceprevir. Your body normally pumps some of the relugolix back out through a kind of gatekeeper called P-gp. Boceprevir slows down that gatekeeper, so more relugolix can build up in your body. Higher levels mean a greater chance of side effects like hot flashes, tiredness, or effects on blood pressure and blood sugar.
The good news is that this is very manageable. Your care team may separate the timing of your doses, watch you more closely, or adjust your plan. Please don't stop or change either medicine on your own. Just check in with your pharmacist or doctor so they can guide you.
Effect: Increased relugolix exposure. Boceprevir inhibits P-gp-mediated efflux of relugolix (a P-gp substrate), raising its systemic exposure and adverse-reaction risk.
Direction/magnitude: Increased relugolix AUC/Cmax. A study with erythromycin (P-gp inhibitor) showed 3.5-fold AUC and 2.9-fold Cmax increases; boceprevir is expected to act similarly. Evidence: probable. Onset unspecified.
Management:
- Avoid coadministration where possible.
- If unavoidable, give relugolix first, separate by at least 6 hours, monitor for adverse effects more frequently.
- 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 combination 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 no less than 6 hours between doses, 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, with relugolix resumed once the P-gp inhibitor has been stopped. Should relugolix be held for more than 7 days, restart it using a loading dose of 360 mg on the first day, followed by 120 mg once daily thereafter. In a drug interaction study, giving relugolix (P-gp substrate) together with erythromycin (P-gp inhibitor) raised relugolix AUC and Cmax 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 manageable, and your care team has clear options:
- Keep taking both as prescribed unless your prescriber tells you otherwise.
- Your team may prefer to avoid using them together if there is an alternative.
- If both are needed, they may have you take relugolix first and separate the doses by at least 6 hours, and watch you more closely for side effects.
- For a short course of boceprevir, relugolix is sometimes paused and restarted afterward, with the dose individualized by your team.
Tell your pharmacist or doctor about any new or worsening side effects so they can tailor your plan.
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 relugolix AUC by 3.5-fold and Cmax by 2.9-fold, respectively 1.
Common questions
Can I take Boceprevir and Relugolix together?
Boceprevir can raise relugolix levels and side-effect risk by blocking its P-gp transport, so avoid combining them if possible; if you must use both, your care team will separate dosing and monitor you closely. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Boceprevir 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 Boceprevir and Relugolix interaction managed?
This combination is manageable, and your care team has clear options: Keep taking both as prescribed unless your prescriber tells you otherwise. Your team may prefer to avoid using them together if there is an alternative. If both are needed, they may have you take relugolix first and separate the doses by at least 6 hours, and watch you more closely for side effects. For a short course of bocepre… 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 Boceprevir 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 Boceprevir
Keep reading about Relugolix
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