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Buprenorphine/naloxone sublingual tablets
Buprenorphine acts as a partial mu-opioid receptor agonist while naloxone acts as a mu-opioid receptor antagonist, together providing opioid dependence treatment with abuse-deterrent properties.
Buprenorphine acts as a partial mu-opioid receptor agonist while naloxone acts as a mu-opioid receptor antagonist, together providing opioid dependence treatment with abuse-deterrent properties. Used for Opioid use disorder maintenance treatment, Opioid dependence management.
At a glance
| Generic name | Buprenorphine/naloxone sublingual tablets |
|---|---|
| Also known as | Zubsolv, OX219, BUP |
| Sponsor | Orexo AB |
| Drug class | Opioid agonist-antagonist combination |
| Target | Mu-opioid receptor (buprenorphine partial agonist; naloxone antagonist) |
| Modality | Small molecule |
| Therapeutic area | Psychiatry / Addiction Medicine |
| Phase | Phase 3 |
Mechanism of action
Buprenorphine's partial agonist activity at the mu-opioid receptor produces sufficient opioid effects to prevent withdrawal symptoms while having a ceiling effect that limits euphoria and overdose risk. Naloxone, included in the sublingual formulation, is poorly absorbed sublingually but becomes active if the tablet is injected, blocking opioid effects and discouraging intravenous misuse. This combination is used for maintenance treatment and management of opioid use disorder.
Approved indications
- Opioid use disorder maintenance treatment
- Opioid dependence management
Common side effects
- Headache
- Nausea
- Constipation
- Insomnia
- Sweating
- Dizziness
Key clinical trials
- A Bundled Intervention - Phase 2 (PHASE4)
- Comparing Outpatient Treatment Retention Among Individuals Using Fentanyl Randomized to Low-dose and Direct-to-inject Buprenorphine Initiation (PHASE4)
- Symptom-Inhibited Naloxone Induction (SINI) for Buprenorphine Initiation: A Feasibility Trial (PHASE4)
- Evaluating Buprenorphine/Naloxone Microdosing vs. Standard Dosing in Emergency Departments (PHASE2, PHASE3)
- Comparing Rapid Micro-Induction and Standard Induction of Buprenorphine/Naloxone for Treatment of Opioid Use Disorder (PHASE2)
- Monthly Versus Daily Buprenorphine Formulations for Treatment of Opiate Use Disorder (PHASE4)
- Medication Maintenance Therapy in Community Pharmacy Settings (PHASE2, PHASE3)
- XRB vs. SLB in Jail and at Re-entry: Pilot, Proof of Concept (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |