Last reviewed 2026-04-22 · How we verify

Oxycodone/Naloxone Prolonged Release

Oxycodone/Naloxone Prolonged Release is a Opioid analgesic with abuse-deterrent formulation Small molecule drug developed by Grünenthal GmbH. It is currently FDA-approved for Chronic moderate to severe pain requiring prolonged opioid therapy. Also known as: Targin.

Oxycodone acts as a mu-opioid receptor agonist to provide analgesia, while naloxone is included to reduce the potential for abuse by blocking opioid effects if the tablet is crushed and injected.

Oxycodone acts as a mu-opioid receptor agonist to provide analgesia, while naloxone is included to reduce the potential for abuse by blocking opioid effects if the tablet is crushed and injected. Used for Chronic moderate to severe pain requiring prolonged opioid therapy.

At a glance

Mechanism of action

Oxycodone binds to mu-opioid receptors in the central nervous system to produce pain relief and is formulated as a prolonged-release preparation for chronic pain management. Naloxone, an opioid antagonist, is incorporated at a low dose that is poorly absorbed orally but becomes active if the formulation is tampered with and injected, thereby discouraging abuse while having minimal impact on the therapeutic opioid effect when taken as directed.

Approved indications

• Chronic moderate to severe pain requiring prolonged opioid therapy

Common side effects

• Constipation
• Nausea
• Dizziness
• Drowsiness
• Vomiting
• Headache

Key clinical trials

• Opioid Induced Bowel Dysfunction in Patients Undergoing Cesarean Section (PHASE4)
• Determine the Safety and Efficacy of Oxy/Nal Tablets Compared to Oxy PR in Subjects With Cancer Pain (PHASE3)
• OXN PR Tablet 5/2.5 mg and20/10 mg PK Study in Chinese Moderate to Severe Chronic Non-malignant Patients (PHASE1)
• A Study Comparing Oxycodone to Oxycodone/Naloxone in Moderate to Severe, Chronic Cancer Pain (PHASE2)
• OXN PR vs Placebo in Opioid-naive Subjects Suffering From Severe Pain Due to Bladder Pain Syndrome (BPS) (PHASE2)
• Oxycodone-naloxone Prolonged Release Tablets in Relieving Opioid-related Constipation (PHASE3)
• A Randomised, Double Blind, Placebo and Active Controlled, Double Dummy,Parallel Group Study to Determine the Safety and Efficacy of Oxycodone/Naloxone Prolonged Release Tablets in Subjects With Moderate to Severe, Chronic Nonmalignant Pain (PHASE3)
• A Study to Demonstrate Improvement in Symptoms of Constipation in Subjects That Require Around-the-clock Opioid Pain Killer Therapy (PHASE3)

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Oxycodone/Naloxone Prolonged Release CI brief — competitive landscape report
• Oxycodone/Naloxone Prolonged Release updates RSS · CI watch RSS
• Grünenthal GmbH portfolio CI

Frequently asked questions about Oxycodone/Naloxone Prolonged Release

Related

• Drug class: All Opioid analgesic with abuse-deterrent formulation drugs
• Target: All drugs targeting Mu-opioid receptor (oxycodone); opioid receptors (naloxone antagonism)
• Manufacturer: Grünenthal GmbH — full pipeline
• Therapeutic area: All drugs in Pain Management
• Indication: Drugs for Chronic moderate to severe pain requiring prolonged opioid therapy
• Also known as: Targin

Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing