Buprenorphine and Tazemetostat: 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
Buprenorphine
Tazemetostat
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.
What's going on: Tazemetostat (Tazverik) can speed up the liver enzyme that breaks down buprenorphine (Belbuca, BuTrans, Sublocade, and others). When that enzyme works faster, your body clears the buprenorphine more quickly, so there may be less of it in your system.
For you, that could mean your pain relief or your opioid-use-disorder treatment doesn't work as well as it should, and you might notice symptoms creeping back or even mild withdrawal feelings. The good news is this is very manageable. Don't change anything on your own, but do let your pharmacist or doctor know you take both so they can watch how you're doing and adjust your dose if needed.
Mechanism: Tazemetostat is a moderate CYP3A4 inducer. Buprenorphine is a CYP3A4 substrate (and active drug, not a prodrug), so induction increases its metabolism and lowers systemic exposure.
Direction/magnitude: Reduced buprenorphine AUC/Cmax and potentially reduced analgesic or maintenance efficacy. In a dedicated study, tazemetostat 800 mg BID decreased midazolam AUC 40% and Cmax 21%.
- Evidence: probable; onset unspecified.
- Severity: major.
- Management: Monitor for loss of analgesia or emerging withdrawal/craving. Buprenorphine dose may need individualized upward titration; reassess after tazemetostat is discontinued as exposure may rise again.
What happens
Reduced CYP3A substrate exposure and reduced efficacy of CYP3A substrate
Interaction Deep Dive
When tazemetostat is taken alongside CYP3A substrates, the exposure to those substrates may fall, which can diminish their effectiveness. A drug interaction study in patients showed that giving tazemetostat 800 mg twice daily together with oral midazolam (a sensitive CYP3A substrate) lowered the AUC of midazolam by 40% and its Cmax by 21%1.
Why it happens (mechanism)
Induction of CYP3A-substrate metabolism by tazemetostat
How to manage this interaction
Keep taking both medications as prescribed unless your care team tells you otherwise. This interaction can be handled with a few practical steps:
- Your prescriber may monitor you more closely for signs that buprenorphine isn't working as well, such as returning pain, cravings, or mild withdrawal symptoms.
- Your buprenorphine dose may need to be adjusted and individualized by your care team.
- If tazemetostat is later stopped, your team may need to re-check your buprenorphine dose again.
What to do: Tell your pharmacist and prescriber you take both, and report any new pain, cravings, or withdrawal feelings promptly.
Management is individual — confirm any change with your pharmacist or prescriber.
Literature reports
1 report — tap to read
a) In a study evaluating drug interactions, giving tazemetostat 800 mg twice daily together with oral midazolam (a sensitive CYP3A substrate) in patients reduced the AUC of midazolam by 40% and its Cmax by 21% 1.
Common questions
Can I take Buprenorphine and Tazemetostat together?
Tazemetostat can lower buprenorphine levels and make it less effective, so watch for returning pain or withdrawal symptoms and ask your care team whether your dose needs adjusting. Always confirm with your pharmacist or prescriber before making any change.
How serious is the Buprenorphine and Tazemetostat 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 Buprenorphine and Tazemetostat interaction managed?
Keep taking both medications as prescribed unless your care team tells you otherwise. This interaction can be handled with a few practical steps: Your prescriber may monitor you more closely for signs that buprenorphine isn't working as well, such as returning pain, cravings, or mild withdrawal symptoms. Your buprenorphine dose may need to be adjusted and individualized by your care team. If tazem… 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 Buprenorphine or Tazemetostat 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: TAZVERIK(R) oral tablets, tazemetostat oral tablets. Epizyme Inc (per FDA), Cambridge, MA, 2024. DailyMed
Keep reading about Buprenorphine
Keep reading about Tazemetostat
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.
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