Determination of the Absorption, Metabolism, Excretion and Absolute Bioavailability of SCH 900777 in Healthy, Adult, Male Volunteers (P-05905).

The drug to be given in this study, SCH 900777, is a new, investigational
compound that may eventually be used for the treatment of depression; the new
compound is still under development.
It is expected that SCH 900777 could play a role in correcting the glutamateric
function in the human brain which is disturbed in patients with e.g.
depression and schizophrenia. Glutamate is an essential amino acid (building
stone of proteins) that in the brain serves to exchange information between
neurons. It is believed that a disturbance in this plays a role in patients
suffering from for example depression. It is expected that SCH 900777 has the
potential to become a novel and improved treatment for depression.

part 1: to assess the absolute bioavailability of SCH900777
part 2: to characterize the absorption, metabolism and excretion of SCH 900777
to evaluate the safety and tolerability of SCH 900777 in healthy subjects

Design:
a two-part, fixed-sequence, single-dose, open-label study of [14C]-SCH 900777

Procedures and assessments
Screening and follow-up:
clinical laboratory, vital signs, physical examination, 12-lead ECG, drug
screen; at eligibility screening: medical history, height, weight, elbow
breadth measurement, drug screen, HBsAg, anti HCV and anti-HIV *.


Observation period :
Part 1: one period in clinic from -17 h up to 48 h after drug administration
Part 2: one period in clinic from -17 h up to 144 h (Day 7) after drug
administration

Blood sampling:
Blood sampling:
for pharmacokinetics of SCH 900777 and total radioactivity in plasma: up to 48
hours post oral dose (Part 1)
for pharmacokinetics of SCH 900435 in plasma and total radioactivity in plasma
and whole blood: up to 144 h post-dose (Part 2)
for metabolic profiling: up to 48 h post-dose (Part 2)
for genotyping: pre-dose (Part 1)


Urine sampling:
for pharmacokinetics of SCH 900777, total radioactivity and metabolite
profiling: up to 48 h and then every 24 h interval until discharge; selected
time points may be analyzed for metabolite profiling (Part 2)


Faeces sampling:
for pharmacokinetics of SCH 900777, total radioactivity and metabolite
profiling: up to 48 h and then every 24 h interval until discharge; selected
time points may be analyzed for metabolite profiling (Part 2)


Safety assessments :
adverse events: throughout the study; physical examination: once on Day 4 (Part
1); clinical laboratory: once on Day 4 (Part 1) and once on Day 1 (Part 2);
vital signs: pre-dose and once on Day 4 (Part 1) and once on Day 1 (Part 2);
12-lead ECG: pre-dose and once on Day 4 (Part 1) and pre-dose (Part 2)


Bioanalyse:
Analyse van SCH 900777 in plasma, urine en feces met een gevalideerde methode
door de sponsor
Analyse van de totale radioactiviteit in plasma, volbloed, urine en feces met
een gevalideerde methode door PRA
Metabolische profilering door de sponsor

Study Medication
Active substance: SCH 900777 and [14C]-SCH 900777

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