Relugolix and Deutivacaftor: 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
Deutivacaftor
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.
Here's what's going on: Relugolix (Orgovyx) is cleared from your body with the help of a kind of "pump" in your gut called P-gp. Deutivacaftor can slow that pump down. When the pump slows, less relugolix gets pushed out, so more of it builds up in your body. More relugolix means a higher chance of side effects.
The good news is that your care team can manage this. They may space the two medicines apart, watch you a little more closely, or adjust your plan. Please don't stop or change either medicine on your own - just talk with your pharmacist or doctor so they can keep you safe.
Mechanism: Deutivacaftor inhibits P-gp-mediated efflux of relugolix (a P-gp substrate), increasing relugolix exposure. Neither drug here acts as a prodrug in this pathway, so the effect is straightforward: higher relugolix AUC/Cmax and increased risk of relugolix-related adverse reactions.
- Magnitude: By analogy to erythromycin (P-gp inhibitor), relugolix AUC increased ~3.5-fold and Cmax ~2.9-fold.
- Evidence: Probable. Onset: unspecified.
- Management: Avoid coadministration if possible. If unavoidable, give relugolix first, separate by at least 6 hours, and monitor for adverse reactions more frequently. Short courses of P-gp inhibitor may allow relugolix interruption up to 2 weeks; if interrupted >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 may 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 a gap of at least 6 hours between doses, and increase the frequency of monitoring for adverse reactions12. For a brief course of certain P-gp inhibitors, relugolix therapy may be paused for up to 2 weeks. Relugolix should be resumed once the P-gp inhibitor has been stopped. Should relugolix be interrupted for longer than 7 days, it should be reinitiated with a 360 mg loading dose 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
What your care team may do:
- Try to avoid using the two together when possible.
- If both are needed, have you take relugolix first and separate the doses by at least 6 hours.
- Watch you more closely for relugolix side effects.
- In some cases, briefly pause relugolix during a short course of the other drug and restart it afterward (sometimes with a loading dose your prescriber will set).
What you should do: Keep taking both exactly as prescribed unless your care team tells you otherwise. Let your pharmacist or doctor know you take both so they can tailor the timing, dose, and monitoring for you.
Management is individual — confirm any change with your pharmacist or prescriber.
Literature reports
1 report — tap to read
a) In a study evaluating drug interactions, 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 Deutivacaftor together?
Deutivacaftor can raise relugolix levels and side-effect risk by slowing a transporter that clears it. Avoid combining if possible, and let your care team manage timing, dosing, and monitoring. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Relugolix and Deutivacaftor 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 Deutivacaftor interaction managed?
What your care team may do: Try to avoid using the two together when possible. If both are needed, have you take relugolix first and separate the doses by at least 6 hours. Watch you more closely for relugolix side effects. In some cases, briefly pause relugolix during a short course of the other drug and restart it afterward (sometimes with a loading dose your prescriber will set). 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 Deutivacaftor 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 Deutivacaftor
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