Vimseltinib and Relugolix: 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
Vimseltinib
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 carried through your gut by a kind of pump called P-gp. Vimseltinib (Romvimza) can slow that pump down. When the pump slows, more relugolix can build up in your body, which may raise the chance of side effects.
The good news: this is very manageable. One simple trick your care team may use is spacing the doses, taking vimseltinib at least 4 hours before relugolix. Please don't change anything on your own. Just check in with your pharmacist or doctor and they'll help you take both safely.
Mechanism: Vimseltinib inhibits P-glycoprotein (P-gp)-mediated efflux. Relugolix is a P-gp substrate with low, variable oral bioavailability, so P-gp inhibition can increase its systemic exposure (AUC/Cmax) and the risk of concentration-related adverse effects.
Direction: increased relugolix exposure (neither drug is a prodrug here).
- Severity/evidence: major; probable substantiation.
- Management: Avoid concomitant use where possible. If unavoidable, administer vimseltinib at least 4 hours prior to relugolix to reduce luminal interaction.
- Monitor: for relugolix-related adverse effects; dosing may be individualized by the care team.
What happens
Increased risk of P-gp substrate exposure
Interaction Deep Dive
Coadministration of vimseltinib with P-gp substrates should be avoided, because it can raise the exposure of the P-gp substrate. When such combined use is unavoidable, administer vimseltinib no less than 4 hours before the P-gp substrate1.
Why it happens (mechanism)
Inhibition of P-gp-mediated efflux transport by vimseltinib
How to manage this interaction
What your care team may do:
- Try to avoid using the two together when another option is reasonable.
- If both are needed, use timing separation, taking vimseltinib at least 4 hours before relugolix.
- Watch you more closely for relugolix side effects, and adjust and individualize your dosing as needed.
What you should do: Keep taking both exactly as prescribed and do not stop or change doses on your own. Tell your pharmacist or prescriber that you take both, and ask how to space them 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) In a drug interaction study, dabigatran (a P-gp substrate) is projected to show a 2- to 3-fold rise in AUC (0 to inf) and Cmax when used together with vimseltinib 30 mg twice weekly. When dabigatran is given 4 hours after administration of vimseltinib 30 mg twice weekly, its Cmax and AUC (0 to inf) are projected to increase up to 1.3-fold 1.
Common questions
Can I take Vimseltinib and Relugolix together?
Vimseltinib can raise relugolix levels by blocking the P-gp pump, so your team may avoid the combo or have you take vimseltinib at least 4 hours before relugolix. Don't change anything on your own; confirm the plan with your pharmacist or doctor. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Vimseltinib and Relugolix 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 Vimseltinib and Relugolix interaction managed?
What your care team may do: Try to avoid using the two together when another option is reasonable. If both are needed, use timing separation, taking vimseltinib at least 4 hours before relugolix. Watch you more closely for relugolix side effects, and adjust and individualize your dosing as needed. What you should do: Keep taking both exactly as prescribed and do not stop or change doses on your ow… 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 Vimseltinib or Relugolix 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 (1)
- Product Information: ROMVIMZA(TM) oral capsules, vimseltinib oral capsules. Deciphera Pharmaceuticals, LLC (per FDA), Waltham, MA, 2025. DailyMed
Keep reading about Relugolix
Keep reading about Vimseltinib
These medications also interact with supplements
Prescription drugs aren't the whole picture — herbal and dietary supplements can interact with them too. From the evidence-graded Natural Medicines database:
major · moderate · minor — check everything you take with our drug–supplement interaction checker.
Check another combination
Our instant two-drug interaction checker is almost here.
Still have questions about this combination?
Every question gets a real answer from a licensed pharmacist — free, and usually within a day.
Ask the pharmacist