A Study to Determine the Excretion Balance and Pharmacokinetics of 14C-GSK573719

• Status: Completed
• Trial end date: 2011-06-22
• Target enrollment: 0
• Participant gender: Male

Summary

This will be a two-period, open-label study conducted at a single site. Six healthy male subjects will participate in the study to ensure at least four fully evaluable subjects. Each subject will receive a single 1000 μg (microgram) oral dose containing 50 μCi (Micro Curie) of [14C]-GSK573719 and a 65 μg intravenous infusion containing 7.1 μCi of [14C]-GSK573719. Whilst subjects are in-house, urine and faecal samples will be collected for a minimum of 168 hours (7 days) after dosing or for up to 240 hours (10 days) depending on the amounts of radioactivity still being excreted after Day 5. Faecal sample collection may continue at home for up to 14 days. Bile samples will be collected using Entero-Test string sampling of duodenal bile. Whole blood and plasma samples will be collected at various sample times after dosing to measure parent drug (plasma only) and total radiolabelled drug related material (blood and plasma). Urine and faeces aliquots will be taken to measure total radiolabelled drug-related material. Samples of urine, faeces and plasma will be transferred into a separate study to characterize and, where possible, quantify metabolites in these matrices.

• Phase: Phase 1
• Accepts Healthy Volunteers?: Accepts Healthy Volunteers

Details

• Lead Sponsor: GlaxoSmithKline
• Treatments: Pharmaceutical Solutions

Criteria

Inclusion:

AST (Aspartate aminotransferase), ALT (Alanine aminotransferase), alkaline phosphatase and bilirubin ≤ 1.5xULN (Upper limit of normal) (isolated bilirubin >1.5xULN is acceptable if bilirubin is fractionated and direct bilirubin <35%) Healthy, non-smoking male subjects, 30-55 years old inclusive Male subjects with female partners of child-bearing potential must agree to use one of the contraception methods listed in Section 8.1 Body Mass Index (BMI) within the range 18.5-29.0 kg/m2 (inclusive) Capable of giving written informed consent Average QTcF < 450 msec; or QTc < 480 msec in subjects with Bundle Branch Block Available to complete the study A history of regular bowel movements

Exclusion:

A positive pre-study Hepatitis B surface antigen or positive Hepatitis C antibody result within 3 months of screening A positive test for HIV (Human Immunodeficiency Virus) antibody Current or chronic history of liver disease, or known hepatic or biliary abnormalities Any clinically relevant abnormality identified on the screening medical assessment laboratory examination or 12-lead ECG (Electrocardiogram) Subjects with a positive urine test for drugs of abuse or alcohol at screening or prior to study medication administration Positive urine cotinine at screening History of regular alcohol consumption within 6 months of the study Treatment with an investigational drug within 60 days or 5 half-lives preceding the first dose of study medication Subjects who have had exposure to more than four new chemical entities within 12 months prior to the first dosing period Use of prescription or non-prescription drugs, including vitamins, herbal and dietary supplements within 7 days or 5 half-lives prior to the first dose of study medication Subjects who have received prescription medication within 14 days prior to the first dose of study drug. Subjects may still be entered into the study, if the prescription medication will not interfere with study procedures or compromise safety Donation of blood in excess of 500mL within 56 days prior to the first dose of study medication Participation in a clinical trial involving administration of 14C-labelled compound(s) within the last 12 months Subjects who have received a total body radiation dose of greater than 5.0 mSv or exposure to significant radiation in the 12 months prior to this study Previous history of active gastric or duodenal ulcer within 6 months prior to the first dose of study medication Any history of bleeding diathesis A pre-existing condition(s) interfering with normal gastrointestinal (GI) anatomy or motility or other GI dysfunction which may interfere with the absorption, distribution, metabolism or elimination of the study drug Surgical procedures on digestive tract An occupation which requires monitoring for radiation exposure, nuclear medicine procedures or excessive x-rays within the past 12 months History of anaphylaxis or anaphylactoid reactions, severe allergic responses to drugs History of sensitivity to any of the study medications Unwillingness or inability to follow the procedures outlined in the protocol Subject is mentally or legally incapacitated