Relugolix and Vorapaxar: 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
Vorapaxar
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.
You've been prescribed vorapaxar (a blood thinner) and relugolix (used for prostate cancer or certain hormone-related conditions). Vorapaxar can block a pump in your gut called P-gp that normally limits how much relugolix gets into your body. When that pump is slowed, more relugolix can build up, which can raise your chance of side effects.
The good news is this is very manageable. Please keep taking both exactly as prescribed and don't change anything on your own. Talk with your pharmacist or doctor, who can adjust timing, monitor you more closely, or tailor your plan so you stay safe.
Effect: Increased relugolix exposure via vorapaxar inhibition of intestinal P-glycoprotein (P-gp)-mediated efflux. Relugolix is a P-gp substrate; reduced efflux raises its AUC/Cmax and the risk of relugolix-related adverse reactions.
- Direction: Increased relugolix effect/exposure.
- Magnitude: With erythromycin (P-gp inhibitor), relugolix AUC increased 3.5-fold, Cmax 2.9-fold.
- Evidence: Probable; Severity: major; onset unspecified.
- Management: Avoid coadministration if possible. If unavoidable, give relugolix first, separate dosing by at least 6 hours, and monitor more frequently. For short P-gp inhibitor courses, relugolix may be interrupted up to 2 weeks; if held >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 exposure to relugolix may rise, potentially heightening the risk of relugolix-related adverse reactions. 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 up to 2 weeks to allow a brief course of treatment with certain P-gp inhibitors. Once the P-gp inhibitor has been stopped, relugolix can be restarted. Should relugolix be interrupted for more than 7 days, resume it with a 360 mg loading dose on day one, followed by 120 mg once daily thereafter. A drug interaction study showed that 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 interaction is manageable with the help of your care team. Here's what they typically consider:
- Avoiding the combination when a suitable alternative exists.
- If both are needed, taking relugolix first and separating the doses by at least 6 hours.
- Monitoring you more closely for relugolix side effects.
- For a short course of the interacting drug, relugolix may be paused and later restarted (with a loading dose if it was held more than 7 days).
Keep taking both as prescribed and don't stop or change anything on your own. Ask your pharmacist or prescriber how best to time your doses and whether any changes are needed.
Management is individual — confirm any change with your pharmacist or prescriber.
Literature reports
1 report — tap to read
a) During a drug interaction study, 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 Relugolix and Vorapaxar together?
Vorapaxar can raise relugolix levels by blocking its P-gp transport, increasing side-effect risk. Don't change anything yourself; ask your pharmacist or doctor about spacing doses and monitoring. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Relugolix and Vorapaxar 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 Vorapaxar interaction managed?
This interaction is manageable with the help of your care team. Here's what they typically consider: Avoiding the combination when a suitable alternative exists. If both are needed, taking relugolix first and separating the doses by at least 6 hours. Monitoring you more closely for relugolix side effects. For a short course of the interacting drug, relugolix may be paused and later restarted (with… 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 Vorapaxar 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 Vorapaxar
Keep reading about Relugolix
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Prescription drugs aren't the whole picture — herbal and dietary supplements can interact with them too. From the evidence-graded Natural Medicines database:
major · moderate · minor — check everything you take with our drug–supplement interaction checker.
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