Last updated: 11/07/2018 07:15:35
A study to evaluate the pharmacokinetics and absolute bioavailability of GSK962040 given as an oral dose simultaneously with an intravenous microtracer dose of [14C]-GSK962040 in healthy volunteers
Clinicaltrials.gov ID
EudraCT ID
EU CT Number
Not applicable
Trial status
Completed
Completed
Trial overview
Official title: A single dose, open label, nonrandomized, study to evaluate the pharmacokinetics and absolute bioavailability of GSK962040 given as an oral dose simultaneously with an intravenous microtracer dose of [14C]-GSK962040 in healthy volunteers
Trial description: The purpose of this study is to determine the absolute oral bioavailability and intravenous pharmacokinetics of GSK962040. The oral dose of 50 mg has been selected because it was well tolerated following single oral administration and it is considered to be within therapeutic dose range. The need to characterize the intravenous disposition of GSK962040 is in anticipation of drug use in special populations such as critically.
Primary purpose:
Treatment
Trial design:
Single Group Assignment
Masking:
None (Open Label)
Allocation:
Randomized
Primary outcomes:
PK parameters for GSK962040 following i.v. dose: AUC(0-inf), Cmax, tmax, t½, systemic clearance (CL), renal clearance (CLr), metabolic clearance (CLm), volume of distribution (Vss), and mean residence time (MRT).
Timeframe: 14 days
PK parameters following oral dose: AUC(0-inf), AUC(0-t), Cmax, tmax, t½, tlag, CLoral and absolute bioavailability (F).
Timeframe: 14 days
Secondary outcomes:
Adverse Events
Timeframe: 14 days
Urine and fecal recovery of GSK962040 following a single oral and i.v. dose of [14C] GSK962040.
Timeframe: 14 days
Urine, fecal recovery and total recovery of radiocarbon (as a percentage of total radioactive dose in each interval and cumulative)
Timeframe: 14 days
Characterization and semi-quantitation of GSK962040-related metabolites in plasma, urine, and fecal homogenates following a single oral and i.v. dose of [14C] GSK962040.
Timeframe: 14 days
Vital signs
Timeframe: 14 days
ECGs
Timeframe: 14 days
Clinical lab assessments
Timeframe: 14 days
Interventions:
Drug: A
Drug: B
Enrollment:
8
Observational study model:
Not applicable
Primary completion date:
Not applicable
Time perspective:
Not applicable
Clinical publications:
L. Stevens, J. Collier, S. Cozens, B. Squillaci, S. Corless, C. Felgate, M.Wright, M. Young.Application of the Entero-Test bile string for accessing biliary excretion of GSK962040 and it's metabolites in healthy subjects.American Association of Pharmaceutical Scientists - 2012 Annual Meeting & Exposition.2012;
Medical condition
Gastroparesis
Product
camicinal
Collaborators
Not applicable
Study date(s)
June 2010 to September 2010
Type
Interventional
Phase
1
Participation criteria
Sex
Male
Age
18 - 65 years
Accepts healthy volunteers
Yes
- Healthy as determined by a responsible and experienced physician, based on a medical evaluation including medical history, physical examination, laboratory tests and ECG. 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. In any case, liver function tests must be strictly within the normal range at screening.
- Male between 18 and 65 years of age inclusive, at the time of signing the informed consent.
- 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).
Inclusion and exclusion criteria
Inclusion criteria:
- Healthy as determined by a responsible and experienced physician, based on a medical evaluation including medical history, physical examination, laboratory tests and ECG. 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. In any case, liver function tests must be strictly within the normal range at screening.
- Male between 18 and 65 years of age inclusive, at the time of signing the informed consent.
- Subjects must agree to use one of the contraception methods listed in Section 10.1. This criterion must be followed from the time of the first dose of study medication through at least 90 days following the dose of GSK962040.
- Body weight > or = 50 kg and BMI within the range 18.5-29.9 kg/m2 (inclusive).
- Capable of giving written informed consent, which includes compliance with the requirements and restrictions listed in the consent form.
- QTcB or QTcF < 450 msec or QTc<480msec in subjects with Bundle Branch Block based on single or average QTc value of triplicate values obtained over a brief recording period.
- Normal physical examination (physical exam demonstrates no evidence of clinically active disease or physical or mental impairment). A subject with a clinical abnormality may be included only if the Principal Investigator or physician designee considers that the abnormality will not introduce additional risk factors and will not interfere with the study procedures. Consultation with the GSK medical monitor is required before such subjects may be included.
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 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 >21 units. One unit is equivalent to 8 g of alcohol: a half-pint (~240 ml) of beer, 1 glass (125 ml) of wine or 1 (25 ml) measure of 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.
- Participation in a clinical trial involving administration of 14C-labelled compound(s) within the last 3 months.
- 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 90 day period.
- Unwillingness or inability to follow the procedures outlined in the protocol.
- Subject is mentally or legally incapacitated.
- Consumption of red wine, Seville oranges, red wine, grapefruit or grapefruit juice, apple juice, vegetables from the mustard green family (e.g., kale, broccoli, watercress, collard greens, kohlrabi, brussel sprouts, mustard), and charbroiled meats from 7 days prior to the dose of study medication. .
- Radiation exposure from clinical trials, including that from the present study, excluding background radiation but including diagnostic X-rays and other medical exposures, exceeding 5 mSv in the last twelve months or 10 mSv in the last five years.
- Subject has abnormal or altered upper gastrointestinal and/or biliary anatomy.
Trial location(s)
Study documents
Clinical study report
Available language(s): English
Scientific result summary
Available language(s): English
If you wish to request for full study report, please contact - [email protected]
Results overview
Refer to study documents
Recruitment status
Completed
Actual primary completion date
Not applicable
Actual study completion date
2010-01-09
Plain language summaries
Plain language summaries of clinical trial results for Phase 2-4 clinical trials that were initiated on or after January 2022 will be posted by GSK within one year following study completion.
Additional information about the trial
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Additional information
Results for study 114136 can be found on the GSK Clinical Study Register.
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