A Two Cohort Study to Look at the Metabolites of GSK221149, the Metabolism of GSK221149 Administered With a High Fat Meal and With Ketoconazole

This study has been completed.
Sponsor:
Information provided by (Responsible Party):
GlaxoSmithKline
ClinicalTrials.gov Identifier:
NCT01627587
First received: June 14, 2012
Last updated: September 13, 2012
Last verified: September 2012

June 14, 2012
September 13, 2012
December 2011
February 2012   (final data collection date for primary outcome measure)
  • Area under the curve, half life [ Time Frame: From Day 1- Day 11 of the study ] [ Designated as safety issue: No ]
  • Area under the curve, half life, when treate with ketconizole [ Time Frame: Day 1-11 ] [ Designated as safety issue: No ]
Same as current
Complete list of historical versions of study NCT01627587 on ClinicalTrials.gov Archive Site
12 lead ECGs, safety labs, vital signs, heart rate, blood pressure [ Time Frame: Day 1- Day 11 of the study ] [ Designated as safety issue: No ]
Same as current
Not Provided
Not Provided
 
A Two Cohort Study to Look at the Metabolites of GSK221149, the Metabolism of GSK221149 Administered With a High Fat Meal and With Ketoconazole
A Two Cohort, Open-label Study to Evaluate the Pharmacokinetics of GSK2847065, the Metabolite of Retosiban (GSK221149) After Single and Repeat Oral Doses, the Pharmacokinetics of GSK221149 Coadministered With a High Fat Meal, and the Pharmacokinetics of GSK221149 Coadministered With an Inhibitor of CYP3A4 (Ketoconazole)

This is a two part study. Part A of the study will evaluate the metabolites of GSK221149 following single and repeat oral dosing and will also assess the pharmacokinetics of GSK221149 when administered with a potent CYP3A4 inhibitor Ketoconazole. Part B of the study will look at the pharmacokinetics of GSK221149 following a high fat meal.

Not Provided
Interventional
Phase 1
Allocation: Randomized
Endpoint Classification: Pharmacokinetics Study
Intervention Model: Single Group Assignment
Masking: Open Label
Primary Purpose: Basic Science
Obstetric Labour, Premature
  • Drug: GSK221149 750 mg
    Treatment A: 750 mg GSK221149 single dose
  • Drug: Ketoconazole
    Treatment B: 400 mg of Ketoconazole single dose
  • Drug: GSK221149 100 mg
    Treatment C: 100mg of GSK221149 single dose
  • Drug: GSK221149 750 mg Fasted
    Treatment D: 750 mg of GSK221149 administered fasted
  • Drug: GSK221149 750 mg + Food
    Treatment E: 750 mg of GSK221149 administered with a high fat meal
  • Experimental: Ketoconazole-Part A
    Healthy Female volunteers of child bearing potential will receive Treatment A, B and C
    Interventions:
    • Drug: GSK221149 750 mg
    • Drug: Ketoconazole
    • Drug: GSK221149 100 mg
  • Experimental: Food-Part B
    Healthy Female Volunteers of child bearing potential will receive Treament D and E
    Interventions:
    • Drug: GSK221149 750 mg Fasted
    • Drug: GSK221149 750 mg + Food
Not Provided

*   Includes publications given by the data provider as well as publications identified by ClinicalTrials.gov Identifier (NCT Number) in Medline.
 
Completed
46
February 2012
February 2012   (final data collection date for primary outcome measure)

Inclusion Criteria:

  • ALT, alkaline phosphatase and bilirubin less than and equal to 1.5xULN (isolated bilirubin >1.5xULN is acceptable if bilirubin is fractionated and direct bilirubin less than 35%).
  • Single [QTc, QTcB or QTcF] less than 450 msec; or QTc less than 480 msec in subjects with Bundle Branch Block.
  • Healthy as determined by a responsible and experienced physician, based on a medical evaluation including medical history, physical examination, laboratory tests and cardiac monitoring. A subject with a clinical abnormality or laboratory parameters outside the reference range for the population being studied may be included only if the Investigator and the GSK Medical Monitor agree that the finding is unlikely to introduce additional risk factors and will not interfere with the study procedures.
  • Female subjects between 18 and 45 years of age inclusive, at the time of signing the informed consent.
  • A female subject is eligible to participate if she is of: Child-bearing potential and is abstinent or agrees to use one of the contraception methods listed in the protocol for an appropriate period of time (as determined by the product label or investigator) prior to the start of dosing to sufficiently minimize the risk of pregnancy at that point. Female subjects must agree to use contraception until 48 hours post last dose.
  • Body weight greater than 50 kg and BMI within the range 19-29.9 kg/m2 (inclusive).

Exclusion Criteria:

  • A positive pre-study Hepatitis B surface antigen or positive Hepatitis C antibody result within 3 months of screening
  • Current or chronic history of liver disease, or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones).
  • A positive pre-study drug/alcohol/urine cotinine screen.
  • A positive test for HIV antibody.
  • History of regular alcohol consumption within 6 months of the study defined as: an average weekly intake of greater than 7 drinks for females. One drink is equivalent to 12 g of alcohol: 12 ounces (360 ml) of beer, 5 ounces (150 ml) of wine or 1.5 ounces (45 ml) of 80 proof distilled spirits.
  • The subject has participated in a clinical trial and has received an investigational product within the following time period prior to the first dosing day in the current study: 30 days, 5 half-lives or twice the duration of the biological effect of the investigational product (whichever is longer).
  • Exposure to more than four new chemical entities within 12 months prior to the first dosing day.
  • Unable to refrain from the use of prescription or non-prescription drugs, including vitamins, herbal and dietary supplements (including St John's Wort) within 7 days (or 14 days if the drug is a potential enzyme inducer) or 5 half-lives (whichever is longer) prior to the first dose of study medication, unless in the opinion of the Investigator and GSK Medical Monitor the medication will not interfere with the study procedures or compromise subject safety.
  • History of sensitivity to any of the study medications, or components thereof or a history of drug or other allergy that, in the opinion of the investigator or GSK Medical Monitor, contraindicates their participation.
  • Where participation in the study would result in donation of blood or blood products in excess of 500 mL within a 56 day period.
  • Pregnant females as determined by positive serum hCG test at screening or prior to dosing.
  • Lactating females.
  • Unwillingness or inability to follow the procedures outlined in the protocol.
  • Subject is mentally or legally incapacitated.
  • Urinary cotinine levels indicative of smoking or history or regular use of tobacco- or nicotine-containing products within 6 months prior to screening.
  • Unable to refrain from consumption of red wine, seville oranges, grapefruit or grapefruit juice and/or pummels, exotic citrus fruits, grapefruit hybrids from 7 days prior to the first dose of study medication.
Female
18 Years to 45 Years
Yes
Contact information is only displayed when the study is recruiting subjects
United States
 
NCT01627587
115893
No
GlaxoSmithKline
GlaxoSmithKline
Not Provided
Study Director: GSK Clinical Trials GlaxoSmithKline
GlaxoSmithKline
September 2012

ICMJE     Data element required by the International Committee of Medical Journal Editors and the World Health Organization ICTRP