A multi-center, single-dose, open-label, randomized, parallel group study to investigate the reduction of initial taspoglutide Cmax after administration of 20 mg taspoglutide 10% Sustained Release Formulation (SRF) using three modified formulations as compared to the current Phase 3 formulation in healthy volunteers.

The drug to be given, taspoglutide, is a new, investigational compound that may
eventually be used for the treatment of diabetes mellitus type 2. The study
drug is still in the development phase. Current therapies for diabetes mellitus
type 2 are often inefficient in controlling glucose levels because they have an
effect on only one or a few of the underlying defects. In addition, some of the
antidiabetic medications are associated with undesirable side-effects.
Moreover, some medications can not be used in some patients or require specific
monitoring. Thus, there is a need for new antidiabetic therapies that are both
more effective and better tolerated than currently available antidiabetic
medications.
Taspoglutide is a novel compound, similar to a hormone in the body that is
involved in regulating blood glucose levels. Previous studies with taspoglutide
have already shown a sustained effect on lowering blood glucose levels.
However, the formulation used until now did cause gastrointestinal complaints
in some cases. The purpose of this study is to assess different formulations of
taspoglutide in order to find an optimal formulation for the treatment of
diabetes mellitus type 2.

Primary:
to assess the reduction of initial study drug Cmax after administration of 20
mg study drug 10% SRF using three modified formulations as compared to the
current Phase 3 formulation in healthy volunteers.

Secondary:
to assess the safety and tolerability of 20 mg study drug administered as 10%
SRF using three modified formulations as compared to the current Phase 3
formulation in healthy volunteers.
to investigate the pharmacokinetics of study drug after administration of 20 mg
study drug 10% SRF using three modified formulations as compared to the current
Phase 3 formulation in volunteers.
to determine the effect of study drug on fasting glucose concentrations after
administration of 20 mg study drug administered as 10% SRF using three modified
formulations as compared to the current Phase 3 formulation in healthy
volunteers.
to investigate the impact of injection speed on the pharmacokinetics of study
drug.

Design:
a single-dose, open-label, randomized, parallel group study in five groups of
twenty healthy subjects (at least 40% of each gender) each receiving a single
subcutaneous injection of study drug, the last group (E) can be dosed only
after the first four groups (A-D) have completed the first eight days of
treatment

Procedures and assessments
Screening and follow up:
The screening will include a physical examination including measurement of
blood pressure, pulse rate, oral temperature, anti-study drug antibodies,
height, weight and waist/hip circumference, a heart trace (electrocardiogram)
recording, and a number of blood and urine tests. You will also be screened for
drugs of abuse, alcohol, Hepatitis B and C, and HIV (= AIDS test). In case of
female participants a pregnancy test will be performed.

Observation period:
one period in clinic from -17 h up to 24 h after drug administration on Day 1
followed by ambulatory visits on Days 3, 4, 6, 8, 10, 12, 15, 17, 19, 22, 24,
26, 29, 36, 43, 50, 57*, 64*, 71*, 78* and 85* (* ambulatory visits might not
be necessary in case study drug BLQ values in three consecutive plasma samples
after Day 57)

Blood samples:
for pharmacodynamics of fasting plasma glucose concentrations: pre-dose, 24 h
post dose and once on Days 3, 4, 6, 8, 10, 12, 15, 17, 19, 22, 24, 26, 29, 36,
43, 50, 57, 64, 71, 78* and 85* (* dependent on study drug plasma levels, see
above)
for pharmacokinetics of the study drug in plasma: pre-dose, at 0.5, 0.75, 1, 2,
3, 4, 5, 6, 7, 8, 9, 10, 12, 14 and 24 h post dose and once on Days 3, 4, 6, 8,
10, 12, 15, 17, 19, 22, 24, 26, 29, 36, 43, 50, 57, 64, 71, 78* and 85* (*
dependent on study drug plasma levels, see above)
for anti-study drug antibodies: once on Days 22 and 50

Safety assessments:
adverse events; throughout the study; vital signs and 12-lead ECG: pre-dose and
4, 8 and 24 h post dose and once on Days 8, 15, 22, 29 , 36, 50, 64 and 78;
clinical laboratory: 24 h post dose and once on Days 8, 15, 22, 29, 36, 50, 64
and 78

Bioanalysis:
analysis of study drug plasma samples using a validated method by Sponsor
analysis of anti-study drug antibodies samples using a validated method by
Sponsor
analysis of fasting plasma glucose concentrations using a validated method by
Sponsor

Taspoglutide injection

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