A HUMAN (PHASE 0) SINGLE MICRODOSE METABOLIC PROFILING STUDY OF [14C]-GMC-252 IN HEALTHY MALE SUBJECTS

The drug to be given GMC-252 is a new, investigational compound that may
eventually be used for the treatment of Diabetes Mellitus Type II. GMC-252 is a
chemical structure that combines the chemical properties of diflunisal and
N-acetylcysteine, a combination which is known to effectively treat Diabetes
Mellitus Type II in pre-clinical studies. Diflunisal is a known drug with
anti-inflammatory activity. N-acetylcysteine is a known drug with antioxidant
activity. This chemical combination is expected to be more effective and safe
than the combination of the two separate drugs.

to confirm that GMC 252 is absorbed in humans
to determine in humans whether GMC 252 is cleaved, yielding diflunisal and
N-acetylcysteine (NAC)
to determine whether additional metabolites are formed with GMC-252 compared
with diflunisal and NAC

Design:
An open-label, non-randomised study.

Procedures and assessments
Screening:
Medical history, demographic data (including body weight and height), clinical
laboratory, alcohol and drug screen,
HBsAg, anti HCV, anti-HIV 1/2, vital signs, 12-lead electrocardiogram (ECG),
physical examination, adverse events from
the signing of the Informed Consent Form, previous and concomitant medication.

Admission:
Drug and alcohol screen, AEs and concomitant medication.

Study drug administration:
Period 1: 60 micropgram [14C]-diflunisal and 40 microgram [14C]-NAC (stabilised
with EDTA)
Period 2: 100 microgram [14C]-GMC-252 lysine salt

Follow-up:
Clinical laboratory, vital signs, ECG, physical examination, AEs and
concomitant medication.

Observation period:
For both periods up to 72 h after drug administration

Blood sampling:
for PK and metabolic profiling of the studydrug and for total radioactivity in
plasma: up to 72 h post-dose

Urine sampling:
- for PK and metabolic profiling of the studydrug and for total radioactivity
in urine: up to 48-72 h post-dose

Safety assessments:
AEs: recorded from the time the Informed Consent Form is signed until
completion of the final visit; concomitant
medication; clinical laboratory: screening, each period at pre-dose and at 72 h
post-dose and at the follow-up visit; vital
signs: each period at pre-dose and up to 72 h post-dose; 12 lead ECG: each
period at pre-dose and up to 72 h post-dose
and at the follow-up visit; physical examination: at screening and at the
follow-up visit.

Bioanalysis:
Analysis of plasma and urine samples for the studydrug and total radioactivity
by the Sponsor using a validated
accelerator mass spectrometry (AMS) method.

Procedures: pain, light bleeding, heamatoma, possibly an infection.