To Assess the Excretion Balance and Pharmacokinetics of a Single Oral Dose of [14C]GW856553 in Healthy Adult Males

NCT00599612 | Completed Phase 1

• 1 other identifier: 107806
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

Pulmonary Disease, Chronic Obstructive

Keywords

GW856553,; radiolabel; ADME,

Outcome Measures

Primary Outcomes (1)

• Percentage of the total radioactive dose administered over time

  The urinary and fecal cumulative excretion will be analyzed.

  Up to 10 days

Secondary Outcomes (23)

• Area under the concentration time curve (AUC) from time zero to infinity (AUC[0-inf]) of total drug

  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

  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

  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

  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

  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

Study Arms (1)

Healthy male volunteers

EXPERIMENTAL

Six healthy male volunteers aged between 30-60 years old will be recruited for this study,

Drug: GW856553

Interventions

GW856553 DRUG

A dose of 10mg GW856553 containing 50µCi of \[14C\]GW856553 will be delivered as 100mL of a 0.1mg/mL GW856553/0.5 µCi/mL oral solution.

Healthy male volunteers

Eligibility Criteria

• Age: 30 Years - 60 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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.

You may not qualify if:

• 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.

Sponsors & Collaborators

• GlaxoSmithKline: lead

Study Sites (1)

GSK Investigational Site

Edinburgh, EH33 2NE, United Kingdom

Location

MeSH Terms

Conditions

Pulmonary Disease, Chronic Obstructive

Interventions

6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-N-(2,2-dimethylprpyl)-3-pyridinecarboxamide

Condition Hierarchy (Ancestors)

Lung Diseases, Obstructive; Lung Diseases; Respiratory Tract Diseases; Chronic Disease; Disease Attributes; Pathologic Processes; Pathological Conditions, Signs and Symptoms

Study Officials

• GSK Clinical Trials

  GlaxoSmithKline

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: January 11, 2008
• First Posted: January 24, 2008
• Study Start: January 17, 2008
• Primary Completion: February 18, 2008
• Study Completion: February 18, 2008
• Last Updated: August 4, 2017

Record last verified: 2017-08

Locations

GB (1)