Last reviewed 2026-04-22 · How we verify

Prolonged-release oxycodone/naloxone

Prolonged-release oxycodone/naloxone is a Opioid analgesic with abuse-deterrent formulation Small molecule drug developed by Kati Järvelä. It is currently FDA-approved for Moderate to severe chronic pain requiring around-the-clock opioid therapy.

Oxycodone acts as a mu-opioid receptor agonist for pain relief, while naloxone is an opioid antagonist included to reduce abuse potential by blocking euphoric effects if the formulation is tampered with.

Oxycodone acts as a mu-opioid receptor agonist for pain relief, while naloxone is an opioid antagonist included to reduce abuse potential by blocking euphoric effects if the formulation is tampered with. Used for Moderate to severe chronic pain requiring around-the-clock opioid therapy.

At a glance

Mechanism of action

The combination leverages oxycodone's potent analgesic properties through mu-opioid receptor activation in the central nervous system. Naloxone is co-formulated at a ratio designed to remain inactive during normal oral administration (due to poor oral bioavailability and first-pass metabolism) but becomes active if the tablet is crushed or dissolved, thereby antagonizing opioid effects and deterring misuse.

Approved indications

• Moderate to severe chronic pain requiring around-the-clock opioid therapy

Common side effects

• Constipation
• Nausea
• Dizziness
• Somnolence
• 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:

• Prolonged-release oxycodone/naloxone CI brief — competitive landscape report
• Prolonged-release oxycodone/naloxone updates RSS · CI watch RSS
• Kati Järvelä portfolio CI

Frequently asked questions about Prolonged-release oxycodone/naloxone

Related

• Drug class: All Opioid analgesic with abuse-deterrent formulation drugs
• Target: All drugs targeting Mu-opioid receptor (oxycodone); opioid receptors (naloxone antagonism)
• Manufacturer: Kati Järvelä — full pipeline
• Therapeutic area: All drugs in Pain Management
• Indication: Drugs for Moderate to severe chronic pain requiring around-the-clock opioid therapy

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