Human Abuse Potential of the New Opioid Analgesic Molecule NKTR-181 Compared with Oxycodone

Abstract Objective Evaluate the human abuse potential, pharmacokinetics, pharmacodynamics, and safety of NKTR-181, a novel mu-opioid agonist molecule, relative to oxycodone. Design This randomized, single-center, double-blind, active- and placebo-controlled five-period crossover study enrolled healt...

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Bibliographic Details
Published in:Pain medicine (Malden, Mass.) Mass.), 2018-02, Vol.19 (2), p.307-318
Main Authors: Webster, Lynn, Henningfield, Jack, Buchhalter, August R, Siddhanti, Suresh, Lu, Lin, Odinecs, Aleksandrs, Di Fonzo, Carlo J, Eldon, Michael A
Format: Article
Language:English
Subjects:
Addiction
Addictions
Adult
Analgesics
Analgesics, Opioid - pharmacology
Central nervous system
Central nervous system depressants
Chronic pain
Clinical trials
Cross-Over Studies
Double-Blind Method
Drug abuse
Drug addiction
Drug development
Drug dosages
Evidence-based medicine
Female
Health risk assessment
Humans
Male
Medical research
Morphinans - pharmacology
Morphine
Narcotics
Novels
Opioid receptors (type mu)
Opioid-Related Disorders
Opioids
OPIOIDS & SUBSTANCE USE DISORDERS SECTION
Oral administration
Oxycodone
Oxycodone - pharmacology
Pharmacodynamics
Pharmacokinetics
Young Adult
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Summary:Abstract Objective Evaluate the human abuse potential, pharmacokinetics, pharmacodynamics, and safety of NKTR-181, a novel mu-opioid agonist molecule, relative to oxycodone. Design This randomized, single-center, double-blind, active- and placebo-controlled five-period crossover study enrolled healthy, adult, non–physically dependent recreational opioid users. Setting Inpatient clinical research site. Subjects Forty-two randomized subjects (73.8% male, 81% white, mean age = 25 years). Methods The primary objective was to evaluate single orally administered 100, 200, and 400 mg NKTR-181 doses in solution compared with 40 mg oxycodone and placebo solutions using the Drug Liking visual analog scale. Secondary measures included the Drug Effects Questionnaire, Addiction Research Center Inventory/Morphine Benzedrine Group Subscale, Price Value Assessment Questionnaire, Global Assessment of Overall Drug Liking, and Take Drug Again Assessment. Central nervous system mu-opioid effects were assessed using pupillometry. The study included qualifying and treatment phases. Subjects received each of the five treatments using a crossover design. Results NKTR-181 at all dose levels had significantly lower Drug Liking Emax than oxycodone (P 
ISSN:1526-2375
1526-4637
DOI:10.1093/pm/pnw344