Healthy Volunteer Study Using 3 Different Formulations of Firategrast
Phase 1
Completed
- Conditions
- Multiple Sclerosis, Relapsing-Remitting
- Interventions
- Registration Number
- NCT01416363
- Lead Sponsor
- GlaxoSmithKline
- Brief Summary
This study will investigate how 3 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 is split into 2 parts. Part 1, involves volunteers receiving 2 new formulations, as a single dose. 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 a proper comparison with the new formulations can be made. The new fomulations will be administered with food and the reference formulation will be given without food. In Part 2, volunteers will receive only one of the 3 formulations as a repeat dose for 7 days. Each of these doses will be given with food.
- Detailed Description
The present study will be conducted in two parts in healthy male volunteers. Part 1 will investigate the pharmacokinetics and tolerability of single doses of firategrast administered as the existing immediate release tablet formulation, as a modified release tablet (3hr) formulation and as a simulated gastro-retentive formulation to be administered via a naso-gastric tube. Subjects will receive each formulation in a randomised 3-way single dose crossover fashion.
Part 2, based on the review of safety, tolerability and pharmacokinetic data from the first two study treatment periods of Part 1, will investigate the pharmacokinetics and tolerability of multiple doses of firategrast administered as the existing immediate release tablet formulation, as a modified release tablet (3hr) formulation and as simulated gastro-retentive formulation to be administered via naso-gastric tube for a period of 7 days.
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- Male
- Target Recruitment
- 38
Inclusion Criteria
- Male aged 18 to 65 yrs inclusive
- Healthy, as determined by study physician
- Capable of giving iformed 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 12 units for males)
- Participation in a clinical trial within 30 days of scheduled first dose
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- CROSSOVER
- Arm && Interventions
Group Intervention Description Treatment Arm CBA: Part 1 Firategrast immediate release tablet Subjects will receive treatment sequence CBA; C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, B : Firategrast 3 hour release tablet 1200 mg once only orally, A : Firategrast immediate release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm BCA: Part 1 Firategrast immediate release tablet Subjects will receive treatment sequence BCA; B : Firategrast 3 hour release tablet 1200 mg once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, A : Firategrast immediate release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm ACB: Part 1 Firategrast immediate release tablet Subjects will receive treatment sequence ACB; A : Firategrast immediate release tablet 1200 milligram (mg) once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, B : Firategrast 3 hour release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm CBA: Part 1 Firategrast modified release tablet Subjects will receive treatment sequence CBA; C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, B : Firategrast 3 hour release tablet 1200 mg once only orally, A : Firategrast immediate release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm ACB: Part 1 Firategrast modified release tablet Subjects will receive treatment sequence ACB; A : Firategrast immediate release tablet 1200 milligram (mg) once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, B : Firategrast 3 hour release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm BAC: Part 1 Firategrast gastro-retentive solution Subjects will receive treatment sequence BAC; B : Firategrast 3 hour release tablet 1200 mg once only orally, A : Firategrast immediate release tablet 1200 mg once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route. There will be a washout period of 5 days between doses. Treatment Arm CAB: Part 1 Firategrast gastro-retentive solution Subjects will receive treatment sequence CAB; C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, A : Firategrast immediate release tablet 1200 mg once only orally, B : Firategrast 3 hour release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm BAC: Part 1 Firategrast modified release tablet Subjects will receive treatment sequence BAC; B : Firategrast 3 hour release tablet 1200 mg once only orally, A : Firategrast immediate release tablet 1200 mg once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route. There will be a washout period of 5 days between doses. Treatment Arm BCA: Part 1 Firategrast gastro-retentive solution Subjects will receive treatment sequence BCA; B : Firategrast 3 hour release tablet 1200 mg once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, A : Firategrast immediate release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm CAB: Part 1 Firategrast immediate release tablet Subjects will receive treatment sequence CAB; C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, A : Firategrast immediate release tablet 1200 mg once only orally, B : Firategrast 3 hour release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm CAB: Part 1 Firategrast modified release tablet Subjects will receive treatment sequence CAB; C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, A : Firategrast immediate release tablet 1200 mg once only orally, B : Firategrast 3 hour release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm ABC: Part 1 Firategrast modified release tablet Subjects will receive treatment sequence ABC; A : Firategrast immediate release tablet 1200 mg once only orally, B : Firategrast 3 hour release tablet 1200 mg once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route. There will be a washout period of 5 days between doses. Treatment Arm ABC: Part 1 Firategrast immediate release tablet Subjects will receive treatment sequence ABC; A : Firategrast immediate release tablet 1200 mg once only orally, B : Firategrast 3 hour release tablet 1200 mg once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route. There will be a washout period of 5 days between doses. Treatment Arm ACB: Part 1 Firategrast gastro-retentive solution Subjects will receive treatment sequence ACB; A : Firategrast immediate release tablet 1200 milligram (mg) once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, B : Firategrast 3 hour release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm BAC: Part 1 Firategrast immediate release tablet Subjects will receive treatment sequence BAC; B : Firategrast 3 hour release tablet 1200 mg once only orally, A : Firategrast immediate release tablet 1200 mg once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route. There will be a washout period of 5 days between doses. Treatment Arm BCA: Part 1 Firategrast modified release tablet Subjects will receive treatment sequence BCA; B : Firategrast 3 hour release tablet 1200 mg once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, A : Firategrast immediate release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm CBA: Part 1 Firategrast gastro-retentive solution Subjects will receive treatment sequence CBA; C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route, B : Firategrast 3 hour release tablet 1200 mg once only orally, A : Firategrast immediate release tablet 1200 mg once only orally. There will be a washout period of 5 days between doses. Treatment Arm ABC: Part 1 Firategrast gastro-retentive solution Subjects will receive treatment sequence ABC; A : Firategrast immediate release tablet 1200 mg once only orally, B : Firategrast 3 hour release tablet 1200 mg once only orally, C : Firategrast simulated gastro-retentive solution 1200 mg once only by naso-gastric route. There will be a washout period of 5 days between doses. Treatment Arm D: Part 2 Firategrast immediate release tablet Subject will receive D: Firategrast immediate release tablet 600 mg twice daily for 7 days Treatment Arm D: Part 2 Firategrast modified release tablet Subject will receive D: Firategrast immediate release tablet 600 mg twice daily for 7 days Treatment Arm D: Part 2 Firategrast gastro-retentive solution Subject will receive D: Firategrast immediate release tablet 600 mg twice daily for 7 days Treatment Arm E: Part 2 Firategrast immediate release tablet Subject will receive E: Firategrast 3 hour release tablet 1200 mg twice daily for 7 days Treatment Arm E: Part 2 Firategrast modified release tablet Subject will receive E: Firategrast 3 hour release tablet 1200 mg twice daily for 7 days Treatment Arm E: Part 2 Firategrast gastro-retentive solution Subject will receive E: Firategrast 3 hour release tablet 1200 mg twice daily for 7 days Treatment Arm F: Part 2 Firategrast immediate release tablet Subject will receive F: Firategrast simulated gastro-retentive solution 1200 mg twice daily for 7 days Treatment Arm F: Part 2 Firategrast modified release tablet Subject will receive F: Firategrast simulated gastro-retentive solution 1200 mg twice daily for 7 days Treatment Arm F: Part 2 Firategrast gastro-retentive solution Subject will receive F: Firategrast simulated gastro-retentive solution 1200 mg twice daily for 7 days
- Primary Outcome Measures
Name Time Method Pharmacokinetic measures for single and repeat dose Part 1: approx. 4 weeks, Part 2: approx 8 days Cmax of firategrast
PK measures for single and repeat dose Part 1 approx 4 weeks, Part 2 approx 8 days AUC(0-t) of firategrast
Pharmacokinetic measurements for single and repeat dose Part 1: approx 4 weeks, Part 2: approx 8 days AUC(0-24) of firategrast
- Secondary Outcome Measures
Name Time Method Safety & Tolerability in single and repeat doses Part 1: approx. 4 weeks, Part 2: approx 8 days Adverse events, changes iin blood pressure, heart rate, ECGs, Haematology, clinical chemistry and urinalysis
CD34 positive cell count Part 1 only approx 4 weeks as data permit - exploratory measure
Trial Locations
- Locations (1)
GSK Investigational Site
🇦🇺Randwick, New South Wales, Australia