Relugolix and Verapamil: 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
Verapamil
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.
Verapamil can raise the levels of relugolix in your body. Verapamil blocks a 'pump' called P-gp that normally helps push relugolix out of your system. When that pump is slowed down, more relugolix stays in your blood. In one study using another pump-blocker, relugolix levels rose about 3 times higher.
Higher levels can mean a greater chance of side effects like hot flashes, tiredness, or other relugolix-related reactions. The good news is that your care team can manage this by spacing the doses out, watching you more closely, or adjusting your plan. Please keep taking both as prescribed and check in with your pharmacist or doctor.
Effect: Increased relugolix exposure (relugolix is a P-gp substrate; verapamil is a P-gp inhibitor). Neither is a prodrug here, so inhibition raises active relugolix levels.
Mechanism: Inhibition of P-gp-mediated intestinal efflux of relugolix, increasing absorption/exposure.
Magnitude: With erythromycin (P-gp inhibitor), relugolix AUC increased 3.5-fold and Cmax 2.9-fold. Evidence: probable. Severity: major.
- 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 a short P-gp inhibitor course; if interrupted >7 days, restart with 360 mg loading dose then 120 mg once daily.
What happens
Increased relugolix exposure
Interaction Deep Dive
Do not use relugolix (a P-gp substrate) together with P-gp inhibitors, because 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 up to 2 weeks to permit a brief course of specific P-gp inhibitors, with relugolix resumed once the P-gp inhibitor has been stopped. Should relugolix be interrupted for more than 7 days, reinitiate it using 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) 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
What your care team may do:
- Try to avoid using verapamil and relugolix together when another option exists.
- If both are needed, take relugolix first and separate the two doses by at least 6 hours.
- Monitor you more closely for relugolix side effects.
- In some cases pause relugolix during a short course of verapamil, then resume (a loading dose may be used if the pause is more than 7 days).
What you should do: Keep taking both exactly as prescribed and do not stop or change anything on your own. Ask your pharmacist or prescriber how best to space the doses and what side effects to watch for.
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 and Cmax of relugolix by 3.5-fold and 2.9-fold, respectively 1.
Common questions
Can I take Relugolix and Verapamil together?
Verapamil can raise relugolix levels and increase side effects; your care team can manage this by separating doses by at least 6 hours, monitoring you closely, or adjusting your plan. Do not change either medication on your own. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Relugolix and Verapamil 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 Verapamil interaction managed?
What your care team may do: Try to avoid using verapamil and relugolix together when another option exists. If both are needed, take relugolix first and separate the two doses by at least 6 hours. Monitor you more closely for relugolix side effects. In some cases pause relugolix during a short course of verapamil, then resume (a loading dose may be used if the pause is more than 7 days). What you… 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.
From our Q&A
Real reader questions about these medications, each personally answered by our pharmacist:
Questions for your pharmacist
- Does my dose of Relugolix or Verapamil 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 Verapamil
Keep reading about Relugolix
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