A single centre, prospective, randomised, double-blind, placebo controlled,
sequential, dose-escalating phase I study to assess the safety and tolerability of intravenously infused single doses of OPN-305 in healthy subjects.

As this study is the first study in humans, to date adverse effects in man have
not been reported. In previous studies with mice and monkeys with dosing once
weekly at dosages up to 100 mg/kg/week no adverse effects were observed.
With the doses used in this study no serious adverse effects are expected.
However, the possibility that any adverse effects could occur cannot be
entirely excluded. All potential drugs cause to some extent adverse events. One
adverse event that may occur is an increased susceptibility for infections.
This is also the main reason why you will be tested for tuberculosis, as this
disease can become active if you are positive without knowing this. However,
you should take into account that some risks are still unknown at this moment.

Primary :
- to assess the safety and tolerability of a single ascending intravenous iv
infused doses of OPN-305 in healthy subjects
- determination of dose and infusion time for Phase II studies

Secondary :
- to determine the pharmacokinetic profile OPN-305 after a single intravenous
injection in healthy subjects
- to determine the immunogenicity of OPN-305 after a single intravenous
injection in healthy subjects
- to confirm that there are no unexpected changes in plasma inflammatory
cytokines (e.g. TNF*, IL-1*, IL-6 and IFN-*)
- to evaluate the effect of OPN-305 on PD parameters

a randomized, double-blind, placebo-controlled, single-ascending dose study in
three cohorts of six healthy male subjects and two cohorts of eight healthy
male subjects receiving a single iv infusion of OPN-305 or placebo, the first
cohort is staggered in such a manner that two subjects (one verum and one
placebo) are dosed, at least, twenty-four hours prior to the next two subjects
and, at least, twenty-four hours later the remaining two subjects, the other
cohorts are staggered in such a manner that two subjects (one verum and one
placebo) are dosed, at least, twenty-four hours prior to the remaining
subjects

Cohort 1: a single 2-hour iv infusion of 0.5 mg/kg OPN-305 or placebo in the
fasted state
Cohort 2: a single 2-hour iv infusion of 1.5 mg/kg OPN-305 or placebo in the
fasted state
Cohort 3: a single 2-hour iv infusion of 5 mg/kg OPN-305 or placebo in the
fasted state
Cohort 4: a single 1-hour iv infusion of 5 mg/kg OPN-305 or placebo in the
fasted state
Cohort 5: a single 1-hour iv infusion of 10 mg/kg OPN-305 or placebo in the
fasted state

Light bleeding and/or an infection may occur due to the use of the canula.