AN OPEN-LABEL STUDY IN HEALTHY MALE SUBJECTS TO ASSESS THE ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF [14C]-LABELED BIA 9-1067 AND METABOLITES FOLLOWING A SINGLE-DOSE ORAL ADMINISTRATION

The study drug is a new investigational compound that may eventually be used
for the treatment of Parkinson's disease. The study drug is not registered as a
drug but has been given to humans before.
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,
expired air, urine and faeces. The safety and tolerability of the compound will
also be evaluated.

The purpose of the study is to investigate how quickly and to what extent the
study drug is absorbed, distributed, metabolized (broken down) and eliminated
from the body.

Design:
An open-label ADME study in six healthy male subjects receiving a 14C labeled,
single oral dose of the study medication, containing approximately 3.33 MBq
radioacarbon.

Procedures and assessments
Screening and follow-up:
Screening: medical history, physical examination, clinical laboratory (blood
and urine; a.o. alcohol and drug screen, HBsAg, anti HCV, anti-HIV 1/2
Clinical laboratory, vital signs (in triplicate at screening), vital signs and
ECG. Upon admissoin vital signs, ECG and clinical laboratory (blood and urine;
a.o. alcohol and drug screen) will be repeated.

Observation period:
one period in clinic from -17 h up to 240 h (Day 11) after drug administration
on Day 1 followed by six 24 h hospitalizations on Days 14/15, 21/22, 28/29,
42/43, 56/57 and 77/78.

Blood sampling;
for total radioactivity in plasma and for bioanalysis of study drug +
metabolites: pre-dose and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16,
24, 36, 48, 72, 120, 168, 240, 336, 504, 672, 1008, 1344, and 1848 h post-dose
for total radioactivity in whole blood : pre-dose and 1, 4, 12, 24, 48, 72,
120 and 168 h post-dose

Urine sampling:
for analysis of total radioactivity and for bioanalysis of study drug +
metabolites: pre-dose and at intervals 0-6, 6-12, 12-24 h post-dose, followed
by 24-h collections up to morning of Day 11 and 24 h collections on Days 14/15,
21/22, 28/29, 42/43, 56/57 and 77/78

Faeces sampling:
for analysis of total radioactivity and for bioanalysis of study drug +
metabolites: all faeces up to morning of day 11 pooled as 24-hour fractions and
stools before/on days 14/15, 21/22, 28/29, 42/43, 56/57 and 67/68, pooled as
24-hour fractions

Expired air:
for total radioactivity: pre-dose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 48, 72,
120, 168 and 240 h post-dose

Safety assessments:
adverse events: throughout study; vital signs: 2, 4 and 12 h post-dose and once
daily on days 2, 4, 8 and 10; clinical laboratory in the morning of day 2

Bioanalysis:
analysis of study drug + metabolites samples using a validated method by sponsor
analysis of total radioactivity in plasma, whole blood, urine, faeces and
expired air using a validated LCS method by PRA or using AMS by Xceleron (for
samples below LOQ of LSC; to be decided)

Active stubstance: BIA 9-1067 and [14C] BIA 9-1067

In previous clinical studies with BIA 9-1067 in more than 600 healthy
volunteers with single doses up to 1200 mg, once-daily doses up to 30 mg for 28
days or once-daily doses of 50 mg for 18 days, the most important adverse
events reported were: somnolence, headache, dizziness and nausea.
The occurrence of known or other effects cannot be excluded.