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Injectable buprenorphine
Buprenorphine is a partial mu-opioid receptor agonist that binds with high affinity to reduce opioid cravings and withdrawal symptoms while producing a ceiling effect on respiratory depression.
Buprenorphine is a partial mu-opioid receptor agonist that binds with high affinity to reduce opioid cravings and withdrawal symptoms while producing a ceiling effect on respiratory depression. Used for Opioid use disorder (maintenance treatment), Moderate to severe pain (analgesic use).
At a glance
| Generic name | Injectable buprenorphine |
|---|---|
| Also known as | Direct-to-inject, Brixadi, Sublocade, Long-acting injectable buprenorphine, XR-BUP (Brixadi) |
| Sponsor | University of California, San Francisco |
| Drug class | Partial mu-opioid receptor agonist |
| Target | Mu-opioid receptor (OPRM1) |
| Modality | Small molecule |
| Therapeutic area | Psychiatry / Addiction Medicine |
| Phase | FDA-approved |
Mechanism of action
Buprenorphine acts as a partial agonist at the mu-opioid receptor, meaning it produces submaximal effects compared to full agonists like heroin or morphine. This partial agonism provides analgesia and reduces withdrawal symptoms in opioid-dependent patients while having a built-in safety ceiling that limits respiratory depression risk. The injectable formulation allows for sustained therapeutic levels and improved medication adherence in opioid use disorder treatment.
Approved indications
- Opioid use disorder (maintenance treatment)
- Moderate to severe pain (analgesic use)
Common side effects
- Headache
- Nausea
- Constipation
- Dizziness
- Injection site reactions
- Sweating
Key clinical trials
- Integrated Outpatient Treatment of Opioid Use Disorder and Severe Injection Related Infections (PHASE2)
- Evaluation of Tirzepatide as an Adjunct to Buprenorphine for the Treatment of Opioid Use Disorder (PHASE2)
- INDV-6001 Multiple-Dose Pharmacokinetic Study (PHASE2)
- Medication Treatment for Opioid Use Disorder in Expectant Mothers: Conceptual Model Assessments Sub-study
- Medication Treatment for Opioid Use Disorder in Expectant Mothers: Infant Neurodevelopmental Outcomes Sub-study
- Comparing Outpatient Treatment Retention Among Individuals Using Fentanyl Randomized to Low-dose and Direct-to-inject Buprenorphine Initiation (PHASE4)
- A Clinical Trial Comparing Buprenorphine Formulations for High Potency Synthetic Opioid Use (EARLY_PHASE1)
- Symptom-Inhibited Naloxone Induction (SINI) for Buprenorphine Initiation: A Feasibility Trial (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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Injectable buprenorphine CI brief — competitive landscape report
- Injectable buprenorphine updates RSS · CI watch RSS
- University of California, San Francisco portfolio CI