Relugolix and Ticagrelor: 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
Ticagrelor
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.
Here's what's going on. Ticagrelor (Brilinta) can block a 'pump' in your body called P-gp that normally helps move relugolix (Orgovyx) out. When that pump is slowed down, more relugolix stays in your system. In one study with a similar blocker, relugolix levels rose about 3 to 4 times higher.
Higher levels can mean a greater chance of side effects from relugolix. The good news is this is very manageable. Don't stop either medicine on your own. Let your pharmacist or doctor know you take both. They can space out the doses, watch you a bit more closely, or adjust your plan so both drugs work safely for you.
Mechanism: Ticagrelor inhibits P-gp-mediated efflux of relugolix (a P-gp substrate), increasing relugolix systemic exposure. Neither agent is activated by this pathway, so the effect is straightforward accumulation of relugolix and heightened adverse-effect risk.
- Direction/magnitude: Increased relugolix AUC and Cmax. A study with erythromycin (P-gp inhibitor) showed a 3.5-fold AUC and 2.9-fold Cmax increase.
- Evidence: Probable; severity major.
- Management: Avoid concomitant use if possible. If unavoidable, give relugolix first, separate dosing by at least 6 hours, and monitor for 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 a 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 it 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, allow at least 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 is stopped. Should relugolix be 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. A drug interaction study showed that giving relugolix (P-gp substrate) together with erythromycin (P-gp inhibitor) raised relugolix AUC by 3.5-fold and Cmax by 2.9-fold1.
Why it happens (mechanism)
Inhibition of P-gp-mediated efflux transport of relugolix
How to manage this interaction
Keep taking both medicines as prescribed unless your care team tells you otherwise, and make sure they know you're on both.
Your team can manage this in a few ways:
- Avoid the combination when a good alternative exists.
- 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.
- In some cases relugolix may be paused during a short course of the other drug, then restarted (with a loading dose if it was held more than 7 days).
Ask your pharmacist or prescriber which approach fits you best.
Management is individual — confirm any change with your pharmacist or prescriber.
Literature reports
1 report — tap to read
a) A drug interaction study found that 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 Ticagrelor together?
Ticagrelor can raise relugolix levels by blocking a transporter, increasing the risk of relugolix side effects. Don't stop either drug on your own; tell your pharmacist or doctor so they can separate the doses, monitor you, or adjust your plan. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Relugolix and Ticagrelor 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 Ticagrelor interaction managed?
Keep taking both medicines as prescribed unless your care team tells you otherwise, and make sure they know you're on both. Your team can manage this in a few ways: Avoid the combination when a good alternative exists. 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. In some cases relugolix may be paused dur… 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 Ticagrelor 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 Ticagrelor
Keep reading about Relugolix
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