A PHASE 1, THREE-PART, RANDOMIZED, PLACEBO-CONTROLLED, DOSE-ESCALATION STUDY OF THE SAFETY, TOLERABILITY, PHARMACOKINETICS AND FOOD EFFECT OF AQX-1125 IN HEALTHY HUMAN SUBJECTS

The drug to be given,is a new investigational compound that may eventually be
used for the treatment of inflammatory diseases, including asthma.
The study drug activates the action of the protein SHIP1. SHIP1 is a protein in
your body that is involved in the production of cells that are part of the
human immune system. In this way, The study drug can influence the pathogenesis
of several diseases, including allergic inflammation and asthma, acute lung
injury and chronic obstructive pulmonary disease (COPD).

Primary:
To assess the safety and tolerability of single and multiple oral ascending
doses of the study drug in healthy human subjects (Part 1 and Part 2)
To assess the effect of food on the absorption and pharmacokinetic (PK) profile
of the study drug in healthy human subjects (Part 3)
To determine the PK profile after single and multiple oral ascending doses of
AQX 1125 in healthy human subjects (Part 1 and Part 2)

Secondary:
To evaluate the biological activity (pharmacodynamics; PD) of single and
multiple oral ascending doses of the study drug in healthy human subjects (Part
1 and Part 2)
To evaluate the effect of food on the safety and tolerability of the study drug
in healthy human subjects (Part 3)

Design:
A 3-part, randomized, placebo-controlled, single- (Part 1) and
multiple-ascending dose (Part 2) and food-effect (Part 3) study.

Part 1 consists of 2 alternating groups of 8 healthy male and/or female
subjects each receiving a single oral dose of the study drug or placebo (6
active and 2 placebo) in 3 periods; in the first dose level 2 subjects will be
dosed (1 active and 1 placebo) and monitored for 24 hours before the remaining
6 subjects will be dosed.

Part 2 consists of 3 groups of 8 healthy male and/or female subjects each
receiving an oral dose of the study drug or placebo (6 active and 2 placebo)
once daily for 10 days.

Part 3 consists of 1 group of 12 healthy male and/or female subjects in an open
randomized 2-period crossover design with a single oral dose of the study drug
in the fasted or fed state in Period 1 and in the fed or fasted state in Period
2; washout of at least 7 days between the treatments.

Procedures and assessments (screening and follow up):
Clinical laboratory (including clinical chemistry, hematology and urinalysis),
vital signs (including supine systolic and diastolic blood pressure, pulse rate
and oral body temperature), body weight, physical examination, 12 lead
electrocardiogram (ECG), previous and concomitant medication, ophthalmology
examination (during follow-up only).
At eligibility screening only: inclusion/exclusion criteria review,
demographics, medical history, height, drug and alcohol screen, hepatitis B
surface antigen (HBsAg), anti hepatitis C virus (HCV), anti-HIV 1/2 and
pregnancy test (females only).

At admission: Inclusion/exclusion criteria review, drug and alcohol screen,
previous and concomitant medication, vital signs, body weight, physical
examination, 12-lead ECG, clinical laboratory, and pregnancy test (females
only) to be repeated upon each admission; in addition, at admission, an
ophthalmology examination will be done.

Part 1
Observation period: Three periods in clinic, each from -18 h up to 96 h after
drug administration on Day 1. Follow-up on Day 15 (Period 3)

Blood sampling: For PK of AQX-1125 in plasma: pre-dose and 0.5, 1, 2, 4, 6, 12,
16, 24, 48, 72 and 96 h post-dose in each period, and at follow-up
For pharmacodynamic (PD) assays and biomarker assessment: pre-dose and 4 and 24
h post-dose in Period 2, and at follow-up

Safety assessments: Adverse events and previous and concomitant medication:
throughout the study; vital signs: pre-dose and 5, 30, 60 min, 2, 6, 12, 24,
48, 72 and 96 h post-dose in each period; weight: pre-dose and 24 and 48 h
post-dose in each period; physical examination: once on Day 5 (before
discharge) in each period; clinical laboratory: 4, 24 and 48 h post-dose in
each period; 12-lead ECG: pre-dose and 4 and 24 h post-dose and once on Day 5
(before discharge) in each period

Bioanalysis: Analysis of the study drug in plasma is to use validated methods
by PRA. Analysis of potential PD markers is to use qualified methods by PRA

Part 2
Observation period: One period in clinic, from -18 h before drug administration
on Day 1 up to 96 h after drug administration on Day 10. Discharge in morning
of Day 14 and follow-up on Day 28

Blood sampling: For PK of AQX-1125 in plasma: pre-dose and 0.5, 1, 2, 4, 6, 12,
16 and 24 h post-dose on Day 1, pre-dose on Days 4, 6 and 8, pre-dose and 0.5,
1, 2, 4, 6, 12, 16, 24, 48, 72 and 96 h post-dose on Day 10 and at follow-up
For PD assays and biomarker assessment: 4 and 24 h post-dose on Day 10 and at
follow-up

Safety assessments: adverse events and previous and concomitant medication:
throughout the study; vital signs: pre-dose and 5, 30, 60 min, 2, 6, and 12 h
post-dose on Day 1 and pre-dose on Days 2, 3, 5 and 7, pre-dose and 5, 30, 60
min, 2, 6 12, 24, 48, 72 and 96 h post-dose on Day 10; weight: pre-dose on
Days 1, 2, 3, 7, 10 and at approximately the same time on Day 14; clinical
laboratory: 4 h post-dose on Day 1, pre-dose on Days 3, 7, 10 and at
approximately the same time on Day 14; 12-lead ECG: pre-dose and 4 h post-dose
on Days 1, 3, 7, 10 and at approximately the same times on Day 14; physical
examination: once on Days 7 and 14; ophthalmic examination: Day 10

Bioanalysis: Analysis of the study drug in plasma is to use validated methods
by PRA. Analysis of potential PD markers is to use qualified methods by PRA

Part 3
Observation period: Two periods in clinic, each from -18 h before drug
administration on Day 1 up to 96 h post-dose; follow-up on Day 8 of Period 2.

Blood sampling: For PK of AQX-1125 in plasma: pre-dose and 0.5, 1, 2, 4, 6, 12,
16, 24, 48, 72 and 96 h post-dose in each period, and at follow-up

Safety assessments: adverse events and previous and concomitant medication:
throughout the study; vital signs: pre-dose and 5, 30, 60 min, 2, 6, 12 and 24
h post-dose in each period; 12-lead ECG: pre-dose and 4 h post-dose in each
period; clinical laboratory: once on Day 1 of each period

Bioanalysis: Analysis of the study drug in plasma is to use validated methods
by PRA

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