A two-period microdosing study to determine the single-dose pharmacokinetics of ITMN-8187 after intravenous and oral administration in healthy subjects.

The drug to be given is a new, investigational compound that may eventually be
used for the treatment of hepatitis C. The studydrug, a protease inhibitor, is
expected to block an enzyme involved in the replication of the virus. As such
the studydrug may be beneficial for hepatitis C patients.

Primary:
- to determine the pharmacokinetics (PK) of parent drug and total radioactivity
after administration of the studydrug

Secondary:
- to determine the absolute bioavailability of ITMN-8187 after oral
administration
- to investigate the safety and tolerability
- to obtain plasma and urine samples which may be used in further PK and
metabolism profiling evaluation of the studydrug

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.

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

Observation period:
- up to 72 h after drug administration

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

iv infusion
- for PK of the studydrug and for total radioactivity in plasma: up to 72 h
after the end of the infusion

Urine sampling:
- for PK 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.

Active substance: ITMN-8187 (radiolabeled)

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