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Open Label, Healthy Volunteers, Bioequivalence Study With Naloxegol

Phase 1
Completed
Conditions
Opioid Induced Constipation
Interventions
Registration Number
NCT01623609
Lead Sponsor
AstraZeneca
Brief Summary

The purpose of this study is to demonstrate the Bioequivalence, assess food administration on the Pharmacokinetics with naloxegol.

Detailed Description

A Phase I, Randomised, Open-label, 3 way Cross-over Study in Healthy Volunteers to Demonstrate the Bioequivalence of the Naloxegol 25 mg Commercial and Phase III Formulations and to Assess the Effect of Food Administration on the Pharmacokinetics of the Commercial Formulation.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
42
Inclusion Criteria
  • Female non-pregnant, non-lactating.
  • Volunteers with suitable veins for cannulation or repeated venipuncture.
  • Male healthy volunteers should be willing to use barrier contraception ie, condoms, from the first day of dosing until 3 months after dosing with the investigational product.
  • The female partner should use contraception during this period.
Exclusion Criteria
  • History of any clinically significant disease or disorder.
  • Any clinically significant illness, medical/surgical procedure or trauma within 4 weeks of the first administration of investigational product.
  • Volunteers who have smoked or used nicotine products within the previous 3 months from the date of screening.
  • Any clinically significant abnormalities in clinical chemistry, haematology, or urinalysis results as judged by the Investigator .

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
ANaloxegolNaloxol IR tablet 25 mg (naloxegol oxalate) commercial formulation under fasted conditions
CNaloxegolNaloxegol film-coated IR tablet 25 mg Phase III formulation under fasted conditions
BNaloxegolNaloxol IR tablet 25 mg (naloxegol oxalate) commercial formulation under fed conditions
Primary Outcome Measures
NameTimeMethod
Description of the pharmacokinetic (PK) profile for naloxegol in terms of maximum observed plasma concentration (Cmax) and area under the plasma concentration-time curve from time zero extrapolated to infinity (AUC) for each treatment period.Predose,0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, and 48 hours
Secondary Outcome Measures
NameTimeMethod
Description of the safety profile in terms of adverse events, clinical laboratory assessments , vital signs (blood pressure and pulse rate), physical examinations, electrocardiograms, and Columbia-Suicide Severity Rating scale (CSSRS)From baseline day 1 through to Follow-up (Maximum 40 days)
Description of the pharmacokinetic(PK) profile for naloxegol in terms of time to Cmax (tmax), terminal half-life (t1/2λz), terminal rate constant (λz). For each treatment periodPredose,0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, and 48 hours
Description of the pharmacokinetic (PK) profile for naloxegol in terms of area under the plasma concentration-time curve from time zero to the time of the last quantifiable concentration [AUC(0-t)].For each treatment periodPredose,0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, and 48 hours
Description of the pharmacokinetic (PK) profile for naloxegol in terms of area under the plasma concentration-time curve from time zero to 24 hours [AUC(0-24)], apparent oral clearance from plasma (CL/F).For each treatment periodPredose,0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, and 48 hours
Description of the pharmacokinetic (PK) profile for naloxegol in terms of apparent volume of distribution during the terminal phase (Vz/F)For each treatment periodPredose,0.25, 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, and 48 hours

Trial Locations

Locations (1)

Research Site

🇬🇧

London, United Kingdom

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