Relugolix and Lasmiditan: 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
Lasmiditan
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. Lasmiditan (Reyvow), your migraine medicine, can slow down a 'pump' in your body called P-gp that normally helps move relugolix (Orgovyx) out. When that pump is blocked, more relugolix stays in your system than usual. In one study, a similar blocker raised relugolix levels by about 3.5 times.
Higher levels can mean a greater chance of side effects from relugolix. The good news is your care team can manage this by spacing the doses out, watching you a bit more closely, or adjusting your plan. Please don't stop or change either medicine on your own, just check in with your pharmacist or doctor.
Interaction: Lasmiditan inhibits P-gp, reducing efflux of the P-gp substrate relugolix and increasing relugolix systemic exposure. Neither drug is a prodrug; the affected drug (relugolix) accumulates.
- Direction: Increased relugolix AUC/Cmax, higher adverse-reaction risk.
- Magnitude: Extrapolated from erythromycin (P-gp inhibitor): AUC up ~3.5-fold, Cmax up ~2.9-fold.
- Evidence/severity: Probable; rated major. Onset unspecified.
- Management: Avoid if possible. If unavoidable, give relugolix first, separate by >=6 hours, and monitor more frequently. Relugolix may be interrupted up to 2 weeks for short P-gp inhibitor courses; 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 this 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 a 6 hour gap 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 held for more than 7 days, restart it using a 360 mg loading dose on the first day, followed by 120 mg once daily. In a drug interaction study, giving relugolix (P-gp substrate) alongside 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
What your care team may do:
- Try to avoid using these together when possible, or choose an alternative.
- If both are needed, take relugolix (or relugolix/estradiol/norethindrone) first and separate the two by at least 6 hours.
- Monitor you more closely for relugolix side effects.
- For a short course of the P-gp inhibitor, relugolix may be paused for up to 2 weeks, then resumed. If it is held more than 7 days, your team may restart it with a loading dose.
What you should do: Keep taking both exactly as prescribed and let your pharmacist or prescriber know you're on both so they can tailor timing and dosing for you.
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 relugolix AUC by 3.5-fold and Cmax by 2.9-fold, respectively 1.
Common questions
Can I take Relugolix and Lasmiditan together?
Lasmiditan can raise relugolix levels by blocking a transporter, increasing the chance of relugolix side effects. Your care team may avoid the combo, separate doses by at least 6 hours, or monitor you more closely, so keep taking both as prescribed and check in with them. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Relugolix and Lasmiditan 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 Lasmiditan interaction managed?
What your care team may do: Try to avoid using these together when possible, or choose an alternative. If both are needed, take relugolix (or relugolix/estradiol/norethindrone) first and separate the two by at least 6 hours. Monitor you more closely for relugolix side effects. For a short course of the P-gp inhibitor, relugolix may be paused for up to 2 weeks, then resumed. If it is held more than… 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 Lasmiditan 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 Lasmiditan
Keep reading about Relugolix
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