Relugolix and Levacetylleucine: 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
Levacetylleucine
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 body with the help of a transporter called P-gp, which acts like a gatekeeper. Levacetylleucine (Aqneursa) can slow that gatekeeper down. When that happens, more relugolix may stay in your system than usual, which could make relugolix side effects (like hot flashes, fatigue, or diarrhea) more noticeable.
I want to reassure you that this is based on how the drugs work in theory, not on strong real-world reports. Your care team can handle it easily by keeping a closer eye on how you feel. Don't stop either medication on your own. Just let your pharmacist or doctor know you take both.
Mechanism: Levacetylleucine inhibits P-glycoprotein (P-gp)-mediated efflux. Relugolix is a P-gp substrate, so coadministration may increase relugolix exposure (AUC/Cmax) and the risk of substrate-related adverse effects.
- Direction: Increased relugolix effect (neither drug is a prodrug requiring activation).
- Magnitude: Not quantified.
- Onset: Unspecified.
- Evidence: Theoretical.
- Management: Monitor more frequently for relugolix-related adverse reactions (hot flush, fatigue, GI effects, hepatic parameters). Dose may be individualized by the care team if warranted.
What happens
Increased P-gp inhibitor exposure and an increased risk of P-gp substrate-related adverse reactions
Interaction Deep Dive
When levacetylleucine is given together with P-gp substrates, the exposure to those P-gp substrates may rise, which can also heighten the likelihood of adverse reactions associated with the P-gp substrate. During concurrent use with levacetylleucine, watch more closely for adverse reactions related to the P-gp substrate1.
Why it happens (mechanism)
Inhibition of P-gp-mediated efflux transport by levacetylleucine
How to manage this interaction
The good news: this is a manageable interaction, and your care team knows how to handle it.
- Keep taking both relugolix and levacetylleucine exactly as prescribed unless your provider tells you otherwise.
- Your team may simply watch you more closely for relugolix side effects such as hot flashes, tiredness, or stomach upset.
- If side effects show up or worsen, your dose may be adjusted and individualized by your care team.
- Tell your pharmacist and prescriber that you take both drugs, and report any new or bothersome symptoms.
Management is individual — confirm any change with your pharmacist or prescriber.
Common questions
Can I take Relugolix and Levacetylleucine together?
Levacetylleucine may raise relugolix levels a bit by slowing the P-gp transporter, so watch for more relugolix side effects and keep both providers informed; this is a theoretical concern your care team can manage with monitoring. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Relugolix and Levacetylleucine interaction?
It is rated moderate. Can be significant — usually manageable with 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 Levacetylleucine interaction managed?
The good news: this is a manageable interaction, and your care team knows how to handle it. Keep taking both relugolix and levacetylleucine exactly as prescribed unless your provider tells you otherwise. Your team may simply watch you more closely for relugolix side effects such as hot flashes, tiredness, or stomach upset. If side effects show up or worsen, your dose may be adjusted and individual… Management is individual — always follow your own care team's guidance.
How strong is the evidence for this interaction?
The evidence is graded "theoretical". Predicted from the drugs' pharmacology; not yet confirmed in people.
Questions for your pharmacist
- Does my dose of Relugolix or Levacetylleucine 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 anything you'd monitor while I'm on both?
References (1)
- Product Information: AQNEURSA(TM) oral suspension, levacetylleucine oral suspension. IntraBio Inc. (per FDA), Austin, TX, 2024. DailyMed
Keep reading about Relugolix
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