Relugolix and Valbenazine: 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
Valbenazine
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.
Let's talk about taking valbenazine (Ingrezza) together with relugolix (Orgovyx). Valbenazine can slow down a natural "pump" in your body (called P-gp) that helps move relugolix out. When that pump is blocked, more relugolix can build up in your blood. Studies suggest this can raise relugolix levels quite a bit, which can mean more of its side effects.
The good news is this is very manageable. Your care team may adjust the timing of your doses, watch you more closely for side effects, or make other changes. Please don't start, stop, or change either medicine on your own. Just talk with your pharmacist or doctor so they can plan the safest approach for you.
Effect: Increased relugolix exposure via valbenazine's inhibition of P-gp-mediated intestinal efflux of relugolix (a P-gp substrate). Direction is increased relugolix AUC/Cmax and greater risk of relugolix-associated adverse reactions. Neither is functionally a prodrug for this interaction.
Magnitude/evidence: Probable; a study with the P-gp inhibitor erythromycin raised relugolix AUC 3.5-fold and Cmax 2.9-fold. Onset unspecified. Severity: major.
Management:
- Avoid concomitant use where possible.
- If unavoidable, give relugolix (or relugolix/estradiol/norethindrone) first and separate by at least 6 hours.
- Monitor for adverse reactions more frequently.
- Relugolix may be interrupted up to 2 weeks for short P-gp inhibitor courses; if interrupted >7 days, restart with 360 mg loading dose, then 120 mg daily.
What happens
Increased relugolix exposure
Interaction Deep Dive
Do not combine relugolix (a P-gp substrate) with P-gp inhibitors, since doing so 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 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 interrupted for more than 7 days, it should be restarted using a loading dose of 360 mg on the first day, followed by 120 mg once daily thereafter. A drug interaction study showed that giving relugolix (P-gp substrate) together with 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 combination is best avoided when possible, but your care team can manage it safely if you need both.
- Keep taking both exactly as prescribed unless your prescriber tells you otherwise.
- Your team may have you take relugolix first and separate the two medicines by at least 6 hours.
- They may watch you more closely for relugolix side effects.
- In some cases relugolix may be paused briefly and restarted afterward, with dosing individualized by your care team.
Tell your pharmacist or doctor that you take both, and report any new or worsening symptoms 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 the AUC of relugolix by 3.5-fold and its Cmax by 2.9-fold 1.
Common questions
Can I take Relugolix and Valbenazine together?
Valbenazine can raise relugolix levels by blocking P-gp, increasing the risk of relugolix side effects. Don't change anything on your own; ask your care team, who can separate dosing by at least 6 hours and monitor you closely. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Relugolix and Valbenazine 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 Valbenazine interaction managed?
This combination is best avoided when possible, but your care team can manage it safely if you need both. Keep taking both exactly as prescribed unless your prescriber tells you otherwise. Your team may have you take relugolix first and separate the two medicines by at least 6 hours. They may watch you more closely for relugolix side effects. In some cases relugolix may be paused briefly and resta… 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 Valbenazine 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 Valbenazine
Keep reading about Relugolix
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