Healthy Volunteer Pilot Study Using 3 Types of Modified Release Formulations of Firategrast to Investigate How Quickly Absorption From the Digestive System Takes Place.

An Open Label, Randomised Healthy Volunteer Study to Assess the Single Dose Safety and Pharmacokinetics of Three Modified Release Dosage Forms of Firategrast

This study will investigate how 3 new types of drug formulations are absorbed by the body. This study is termed 'open-label', which means volunteers will be aware of which treatment they are receiving. The study involves all volunteers receiving all 3 different formulations, as a single dose, and there is no placebo (dummy-drug; no active ingredient) in this study. Volunteers will also receive a single dose of a formulation used in previous trials (reference formulation), so as a proper comparison with the new formulations can be made. One of the new formulations will also be administered along with food, to assess if the drug performs or is absorbed differently.

Study Overview

• Status: Completed
• Conditions: Multiple Sclerosis, Relapsing-Remitting
• Intervention / Treatment: Drug: B; Drug: C; Drug: D; Drug: A

Detailed Description

The present study will investigate the tolerability and pharmacokinetics of single oral doses of firategrast administered as the existing immediate release tablet formulation and as three modified release tablet formulations designed to release drug over differing relase rates. The range of release rates is expected to give preliminary information on the performance of a matrix modified release formulation for use in future efficacy studies.

Subjects will receive each formulation in the fasted state in a randomised 4-part single dose crossover fashion. Based on the review of pharmacokinetic data from at least the first two study sessions, subjects may also receive a fifth dose of firategrast, administered after a high fat meal. The formulation administered with food will be chosen based upon pharmacokinetic data from previous dose sessions. Doses administered will be different with respect to gender; the doses are expected to result in similar exposures across the genders.

• Study Type: Interventional
• Enrollment (Actual): 20
• Phase: Phase 1

Contacts and Locations

Study Locations

• Australia
  • New South Wales
    • Randwick, New South Wales, Australia, 2031
      • GSK Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 65 years (ADULT, OLDER_ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Male or female, aged 18 to 65 yrs inclusive
• Healthy, as determined by study physician
• Capable of giving informed consent

Exclusion Criteria:

• Positive drugs of abuse result
• Positive for HIV or Hepatitis B and/or C viruses
• History of alcohol consumption in excess of average recommended weekly intake (more than 21 units for males, more than 14 units for females)
• Participation in a clinical trial within 90 days of scheduled first dose

Study Plan

How is the study designed?

Design Details

• Primary Purpose: TREATMENT
• Allocation: RANDOMIZED
• Interventional Model: CROSSOVER
• Masking: NONE

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Firategrast XRA; Low extended release tablet	Drug: B; Low Extended release single dose
Experimental: Firategrast XRB; Medium extended releast tablet	Drug: C; Medium extended release formulation
Experimental: Firategrast XRC; High extended release tablet	Drug: D; High extended release rate single dose
Experimental: Firategrast IR; Immediate Release reference tablet	Drug: A; Single dose treatment IR formulation

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Systemic concentration & AUC of study drug	pre-dose, up to 120 hours after each single dose

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Adverse events		from screening, through study day, and up to follow-up visit. Spontaneous reporting
Systemic concentration & AUC of study drug metabolite		pre-dose, up to 120 hours after each single dose
Vital signs		screening, pre-dose, up-to 15 hours post does, follow-up visit
12-lead Electrocardiogram		screening, pre-dose and up to 8 hours post dose, then at follow-up
Heamatology, clinical chemistry and Uninalysis	Blood samples for standard clinical safety monitoring, and unine samples	screening, predose, up-to 8 hours post dose, follow-up

Collaborators and Investigators

• Sponsor: GlaxoSmithKline

Study record dates

Study Major Dates

• Study Start (Actual): April 19, 2010
• Primary Completion (Actual): July 6, 2010
• Study Completion (Actual): July 6, 2010

Study Registration Dates

• First Submitted: April 14, 2011
• First Submitted That Met QC Criteria: August 25, 2011
• First Posted (Estimate): August 29, 2011

Study Record Updates

• Last Update Posted (Actual): June 20, 2017
• Last Update Submitted That Met QC Criteria: June 19, 2017
• Last Verified: June 1, 2017

More Information

Terms related to this study

• Keywords: Pharmacokinetics; healthy volunteers; modified release; firategrast
• Additional Relevant MeSH Terms: Nervous System Diseases; Immune System Diseases; Demyelinating Autoimmune Diseases, CNS; Autoimmune Diseases of the Nervous System; Demyelinating Diseases; Autoimmune Diseases; Multiple Sclerosis; Multiple Sclerosis, Relapsing-Remitting
• Other Study ID Numbers: 114107