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Oral Naltrexone
Oral naltrexone is an opioid receptor antagonist that blocks the effects of opioids and endogenous opioid peptides in the central nervous system.
Oral naltrexone is an opioid receptor antagonist that blocks the effects of opioids and endogenous opioid peptides in the central and peripheral nervous system. Used for Opioid use disorder (maintenance treatment to prevent relapse), Alcohol use disorder, Chronic pain (off-label, particularly at low doses).
At a glance
| Generic name | Oral Naltrexone |
|---|---|
| Also known as | Revia, Vivitrol, buprenorphine and oral naltrexone followed by Vivitrol, PBO, Vivitrol® |
| Sponsor | New York State Psychiatric Institute |
| Drug class | Opioid receptor antagonist |
| Target | Opioid receptors (mu, delta, kappa) |
| Modality | Small molecule |
| Therapeutic area | Psychiatry / Addiction Medicine / Immunology |
| Phase | FDA-approved |
Mechanism of action
Naltrexone competitively binds to opioid receptors (mu, delta, and kappa) and prevents opioid agonists from activating these receptors. This mechanism is used to reduce cravings and block the rewarding effects of opioids in opioid use disorder, and has also been studied for other conditions including alcohol use disorder and chronic pain when combined with low-dose naltrexone (LDN) formulations.
Approved indications
- Opioid use disorder (maintenance treatment)
- Alcohol use disorder
- Opioid overdose reversal (acute use)
Common side effects
- Nausea
- Headache
- Anxiety
- Insomnia
- Abdominal pain
- Joint and muscle pain
- Hepatotoxicity (at high doses)
Key clinical trials
- Combination Therapy for Alcohol Use Disorder (PHASE2)
- Single Dose Study, Pharmacokinetics of Oxycodone and PF614 Co-Administered With Nafamostat (PF614-MPAR-102) (PHASE1)
- Low Dose Naltrexone (LDN) for Management of Fatigue in Prostate Cancer Patients on Androgen Deprivation Therapy (ADT) (PHASE2)
- Trial of Naltrexone/Bupropion for the Treatment of Methamphetamine Use Disorder (PHASE3)
- Rapid Antidepressant Improvement Secondary to Excitatory Brain Responses (PHASE4)
- Low-Dose Naltrexone For ME/CFS: Dose-Finding (PHASE2)
- A Trial to Investigate the Effects of Cannabidiol Plus Naltrexone on Alcohol Craving in Patients With Alcohol Dependence (PHASE2)
- Low Dose Naltrexone to Improve Physical Health in Patients With Vasculitis (PHASE2)
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:
- Oral Naltrexone CI brief — competitive landscape report
- Oral Naltrexone updates RSS · CI watch RSS
- New York State Psychiatric Institute portfolio CI