An open-label, two period study to determine the excretion balance and pharmacokinetics of 14C-GSK573719, administered as single dose of an oral solution and an intravenous infusion, to
healthy male adults

GSK573719 is a new investigational compound that may eventually be used for the
treatment of Chronic Obstructive Pulmonary Disease (COPD). GSK573719 is not
registered as a drug but has been given to humans before.

The purpose of the study is to investigate how quickly and to what extent
GSK573719 is absorbed, distributed, metabolized (broken down) and eliminated
from the body (this is called pharmacokinetics). The compound to be
administered will be labeled with 14-Carbon (14C) and is thus radioactive. This
enables the investigator to trace the compound in blood, bile, urine and
faeces. The safety and tolerability of the compound will also be evaluated.

Design:
an open-label, two-period, single-dose ADME study in six healthy male subjects
each receiving a single intravenous infusion dose of [14C]-GSK573719
administered over 30 minutes in the first dosing period and a single oral dose
of [14C]-GSK573719 in the second dosing period with a washout of at least 28
days between doses.

Screening and follow up:
clinical laboratory, physical examination, ECG, vital signs; at eligibility
screening: medical history, alcohol urine test, drug screen, HBsAg, anti HCV,
anti-HIV 1/2, urine cotinine, pharmacokinetic blood sample; brief physical
examination, alcohol urine test, drug screen and clinical laboratory to be
repeated upon each admission

Observation period:
two periods in clinic from -17 h up to 168 h after drug administration with a
possible extension to Day 11, subjects can be discharged if 1% or less of the
dose is excreted in a 24 h on Day 6 and Day 7; feaces collection may continue
at home up to Day 14

Blood sampling:
for pharmacokinetics of GSK573719 and metabolites: pre-dose on Day -1, pre-dose
and 0.5, 0.75, 1, 2, 3, 4, 6, 8, 12, 24, 48, 96 and 168 h post-dose
for total radioactivity and metabolite profiling: pre-dose and 0.75, 1, 3, 6
and 24 h post-dose

Urine sampling:
for pharmacokinetics and total radioactivity: pre-dose and intervals 0-24,
24-48, 48-72, 72-96, 96-120, 120-144, 144-168 h post-dose (one aliquot of each
urine collection will be taken for metabolite profiling); urine collection may
continue until Day 11

Feces collection:
for pharmacokinetics and total radioactivity: pre-dose and intervals 0-24,
24-48, 48-72, 72-96, 96-120, 120-144, 144-168 h post-dose (one aliquot of each
faeces collection will be taken for metabolite profiling); faeces collection
may continue until Day 14

Bile sampling:
entero test: in the fasted state from 3.5 h pre-dose until approximately 2.5 h
post-dose on Day 1 in treatment Period 2

Safety assessments:
adverse events: throughout the study; vital signs and ECG: pre-dose and 0.5, 1,
2, 6 and 12 h post-dose

Bioanalysis:
analysis of plasma GSK573719 samples using validated methods by PRA
analysis of total radioactivity in plasma, urine and faeces using validated
methods by PRA
metabolite profiling by Sponsor
analysis of bile samples by Sponsor

active substance: GSK573719 and [14C]-GSK573719

Procedures: pain, licht bleeding, bruses, possible infection.

In previous studies a total of 182 healthy volunteers have received single and
multiple (up to 14 days) dose administrations of GSK573719 up to 1.0 mg daily.
The most important adverse events reported were: headache, coughing, dry mouth
and strange taste.