Last updated: 11/03/2018 09:48:06
To Assess the Excretion Balance and Pharmacokinetics of a Single Oral Dose of [14C]GW856553 in Healthy Adult Males
Clinicaltrials.gov ID
EudraCT ID
EU CT Number
Not applicable
Trial status
Study complete
Study complete
Trial overview
Official title: An open label study to determine the safety, tolerability, excretion balance and pharmacokinetics of [14C]GW856553, administered as a single dose of an oral solution to healthy adult male subjects
Trial description: This will be an open label study conducted at one site. Six healthy male subjects will be enrolled to ensure at least four fully evaluable subjects. Each subject will receive a single 10 milligram (mg) oral dose of GW856553 containing 50 microCi (µCi) of [14C] GW856553. Urine and fecal samples will be collected until 216 hour after dosing but subjects may be discharged after 168 hour if 90% of the dose is recovered and/or <1% of the dose is excreted in a 24 hour period. Blood and plasma will be collected at various sample times after dosing to measure parent drug and total drug-related material. Samples of urine, faeces and plasma will be transferred into a separate study to characterize and quantify metabolites in these matrices. Safety will be assessed by adverse event monitoring, vital signs, electrocardiogram (ECG) and clinical laboratory tests.
Primary purpose:
Treatment
Trial design:
Single Group Assignment
Masking:
None (Open Label)
Allocation:
Non-randomized
Primary outcomes:
Percentage of the total radioactive dose administered over time
Timeframe: Up to 10 days
Secondary outcomes:
Area under the concentration time curve (AUC) from time zero to infinity (AUC[0-inf]) of total drug
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose
Maximum plasma concentration(Cmax) of total drug
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose
AUC from zero to the time of the last measurable concentration (AUC[0-t]) of total drug
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose
First time of occurrence of maximum observed concentration (Tmax) of total drug
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose
Terminal plasma half-life (t1/2) of total drug
Timeframe: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168 hours post-dose
AUC(0-inf) of GW856553
Timeframe: Pre-dose and 1, 4, 12 hours post-dose
AUC(0-inf) of GSK198602
Timeframe: Pre-dose and 1, 4, 12 hours post-dose
Cmax of GW856553
Timeframe: Pre-dose and 1, 4, 12 hours post-dose
Cmax of GSK198602
Timeframe: Pre-dose and 1, 4, 12 hours post-dose
AUC(0-t) of GW856553
Timeframe: Pre-dose and 1, 4, 12 hours post-dose
AUC(0-t) of GSK198602
Timeframe: Pre-dose and 1, 4, 12 hours post-dose
Tmax of GW856553
Timeframe: Pre-dose and 1, 4, 12 hours post-dose
Tmax of GSK198602
Timeframe: Pre-dose and 1, 4, 12 hours post-dose
T1/2 of GW856553
Timeframe: Pre-dose and 1, 4, 12 hours post-dose
T1/2 of GSK198602
Timeframe: Pre-dose and 1, 4, 12 hours post-dose
Number of subjects with Adverse events (AEs) and serious adverse events (SAEs)
Timeframe: Up to 15 days
Number of subjects with abnormal ECG findings
Timeframe: Up to 15 days
Number of subjects with abnormal blood pressure values
Timeframe: Up to 15 days
Number of subjects with abnormal heart rate values
Timeframe: Up to 15 days
Number of subjects with abnormal clinical chemistry parameters
Timeframe: Up to 15 days
Number of subjects with abnormal clinical hematology parameters
Timeframe: Up to 15 days
Number of subjects with abnormal urine analysis parameters
Timeframe: Up to 15 days
Number of subjects with abnormal liver function tests
Timeframe: Up to 15 days
Interventions:
Enrollment:
6
Primary completion date:
Not applicable
Observational study model:
Not applicable
Time perspective:
Not applicable
Clinical publications:
Not applicable
Medical condition
Pulmonary Disease, Chronic Obstructive
Product
losmapimod
Collaborators
Not applicable
Study date(s)
January 2008 to February 2008
Type
Interventional
Phase
1
Participation criteria
Sex
Male
Age
30 - 60 years
Accepts healthy volunteers
Yes
- Healthy male aged between 30 and 60 years inclusive, at the time of screening.
- Body weight >/ 50 kilogram (kg).
- Any clinically relevant abnormality identified on the screening medical assessment, laboratory examination, or ECG (12-lead).
- Significant cardiac, pulmonary, metabolic, renal, hepatic, or gastrointestinal conditions that in the opinion of the investigator and/or GSK medical monitor, places the subject at an unacceptable risk as participant in this trial.
Inclusion and exclusion criteria
Inclusion criteria:
- Healthy male aged between 30 and 60 years inclusive, at the time of screening.
- Body weight >/ 50 kilogram (kg).
- A body mass index (BMI) within the range of 18.5 to 29.9 kg/ meter square (m^2) inclusive.
- Signed and dated written informed consent prior to admission to the study.
- The subject is able to understand and comply with protocol requirements, instructions and protocol-stated restrictions.
Exclusion criteria:
- Any clinically relevant abnormality identified on the screening medical assessment, laboratory examination, or ECG (12-lead).
- Significant cardiac, pulmonary, metabolic, renal, hepatic, or gastrointestinal conditions that in the opinion of the investigator and/or GSK medical monitor, places the subject at an unacceptable risk as participant in this trial.
- QT interval corrected by Bazett's Formula (QTcB) > 450 milliseconds (msecs)
- A definite or suspected personal or family history of adverse reactions or hypersensitivity to the trial drug or to drugs with a similar chemical structure.
- History of regular alcohol consumption exceeding an average weekly intake of > 21 units (or an average daily intake of greater than 3 units). One unit is equivalent to a half-pint [284 milliliter (mL)] of beer/lager; 25mL measure of spirits or 125mL of wine).
- Subjects with a history or presence of gastro-intestinal or renal disease or any other condition known to interfere with the absorption, distribution, metabolism or excretion of drugs.
- Subjects who have consumed grapefruit or grapefruit juice within seven days of the first study day.
- Subjects who have had exposure to more than three new chemical entities within 12 months prior to the first dosing period.
- Subjects who have participated in a trial with a different new chemical entity within 90 days prior to the start of this study.
- If participation in the study will result in the volunteer having donated more than 400mL of blood in the previous 56 days.
- Subjects who have received a total body radiation dose of greater than 5.0 mSv (upper limit of WHO category II) or exposure to significant radiation (e.g. serial X-ray or CT scans, barium meal etc) in the 12 months prior to this study.
- History of elevated blood pressure or blood pressure persistently >140/90 mmHg at screening.
- An unwillingness to abstain from sexual intercourse with pregnant or lactating women; or an unwillingness of the subject to use a condom/spermicide in addition to having their female partner use another form of contraception such as an IUD, diaphragm with spermicide, oral contraceptives, injectable progesterone, sub dermal implants or a tubal ligation if the women could become pregnant from the time of the first dose of the study medication until completion of the follow-up procedures.
- Lack of suitability for participation in this study, for any reason, in the opinion of the investigator.
- Any condition that could interfere with the accurate assessment and recovery of 14C.
- Prescribed or over-the-counter medication within 5 days (or 5 half lives, whichever is longer) prior to the first dosing day, unless the investigator confirms that it will not introduce additional risk or interfere with the study procedures or outcome.
- Liver function tests (ALT, AST, ALP, Gamma GT and bilirubin) > upper limit of normal (ULN) at screening
- Positive urine drug screen
- Positive HIV, Hepatitis B or C result at screening.
- History of use of tobacco- or nicotine-containing products within 6 months of screening or a positive urine cotinine screen (urine cotinine > 250ng/ml).
Trial location(s)
Location
GSK Investigational Site
Edinburgh, United Kingdom, EH33 2NE
Status
Will Be Recruiting
Study documents
Clinical study report
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
Study complete
Actual primary completion date
Not applicable
Actual study completion date
2008-18-02
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
Additional information
Not applicable
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Access to clinical trial data by researchers
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