Abuse Potential Study of ALO-02 (Extended-Release Oxycodone Surrounding Sequestered Naltrexone) Compared with Immediate-Release Oxycodone Administered Orally to Nondependent Recreational Opioid Users

Pain Med. 2017 Jun 1;18(6):1077-1088. doi: 10.1093/pm/pnw178.

Abstract

Objective: To evaluate the abuse potential of ALO-02, an abuse-deterrent formulation comprising pellets of extended-release oxycodone hydrochloride surrounding sequestered naltrexone hydrochloride.

Design: Randomized, double-blind, placebo-/active-controlled, 6-way crossover study, with naloxone challenge, drug discrimination, and treatment phases.

Subjects: Nondependent, recreational opioid users.

Methods: Oral administration of crushed and intact ALO-02, crushed immediate-release (IR) oxycodone, and placebo. Primary endpoints were Drug Liking and High measured on visual analog scales and reported as maximum effect (E max ) and area-under-the-effect-curve from 0 to 2 hours (AUE 0-2h ). Other pharmacodynamic, pharmacokinetic and safety assessments were included.

Results: Drug Liking and High (E max ) for crushed oxycodone IR 40 mg were significantly higher compared with placebo, confirming study validity ( P < 0.0001). Drug Liking and High (E max, AUE 0-2h ) for crushed ALO-02 (40 mg/4.8 mg and 60 mg/7.2 mg) were significantly lower compared to corresponding doses of crushed oxycodone IR (40 and 60 mg; P < 0.0001). Likewise, Drug Liking and High (E max and AUE 0-2h ) for intact ALO-02 60 mg/7.2 mg were significantly lower compared with crushed oxycodone IR 60 mg ( P < 0.0001). Secondary pharmacodynamic endpoints and plasma concentrations of oxycodone and naltrexone were consistent with these results. Fewer participants experienced adverse events (AEs) after ALO-02 (crushed or intact: 71.1-91.9%) compared with crushed oxycodone IR (100%). Most common AEs following crushed ALO-02 and oxycodone IR were euphoric mood, pruritus, somnolence, and dizziness.

Conclusions: The results suggest that ALO-02 (crushed or intact) has lower abuse potential than crushed oxycodone IR when administered orally in nondependent, recreational opioid users.

Keywords: ALO-02; Abuse Deterrent; Abuse Potential; Opioids; Oxycodone.

Publication types

  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Analgesics, Opioid / administration & dosage*
  • Analgesics, Opioid / blood
  • Cross-Over Studies
  • Delayed-Action Preparations / administration & dosage
  • Delayed-Action Preparations / metabolism
  • Double-Blind Method
  • Female
  • Humans
  • Illicit Drugs* / blood
  • Male
  • Naloxone / administration & dosage
  • Naloxone / blood
  • Narcotic Antagonists / administration & dosage
  • Narcotic Antagonists / blood
  • Opioid-Related Disorders / blood
  • Opioid-Related Disorders / diagnosis*
  • Opioid-Related Disorders / drug therapy
  • Oxycodone / administration & dosage*
  • Oxycodone / blood

Substances

  • Analgesics, Opioid
  • Delayed-Action Preparations
  • Illicit Drugs
  • Narcotic Antagonists
  • Naloxone
  • Oxycodone