In this study we will investigate how safe the compound leriglitazone is and how well it is tolerated when it is used by healthy participants.Apart from extensive laboratory and animal testing, leriglitazone has been used in the past both in healthy…
ID
Source
Brief title
Condition
- Other condition
- Central nervous system infections and inflammations
Synonym
Health condition
adrenoleukodystrophy and Friedreich's ataxia
Research involving
Sponsors and support
Intervention
Outcome measures
Primary outcome
Adverse events, clinical laboratory (clinical chemistry, hematology, and
urinalysis), vital signs (systolic and diastolic blood pressure, pulse, body
temperature, and respiratory rate), 12-lead electrocardiogram (heart rate, PR
interval, QRS-duration, QT-interval, and QTcF-interval), and physical
examination.
Secondary outcome
N/A
Background summary
Leriglitazone is a compound that may potentially be used for the treatment of
central nervous system diseases. Leriglitazone binds to and activates PPAR
gamma receptors in brain cells. This causes several positive effects in these
brain cells including restoring energy balance, decreasing stress, improved
neuronal protection and decreasing inflammation. Leriglitazone is also found to
have a protective effect on the blood brain barrier. This barrier is a sort of
filter that separates the brain from the blood (in the body). Studies in
patients with neurological disorders (adrenoleukodystrophy and Friedreich*s
ataxia) who were given leriglitazone showed a clinical benefit in these
patients. Leriglitazone can possibly be used in the future for the treatment of
these diseases of the central nervous system.
Study objective
In this study we will investigate how safe the compound leriglitazone is and
how well it is tolerated when it is used by healthy participants.
Apart from extensive laboratory and animal testing, leriglitazone has been used
in the past both in healthy participants and in patients in clinical trials
proving to be safe and well tolerated.
Leriglitazone is an *active metabolite* of pioglitazone, that means it results
from decomposition during metabolism and in general are very similar compounds.
Pioglitazone is already available on the market and is a well-known drug used
for the treatment of type 2 diabetes.
We also investigate how quick and to what extent leriglitazone is absorbed,
transported, and eliminated from the body (this is called pharmacokinetics)
after oral administration. Only in Part B, oral administration is followed by
an intravenous administration. For this study (Part A and B), leriglitazone is
radioactively labelled with carbon-14 (14C). In this way leriglitazone can be
traced in blood, urine, and feces.
Study design
For the study it is necessary that the volunteer will stay in the research
center for 1 period of 15 days (14 nights). If the stop criteria are not met on
Day 14 the volunteer will have to return for 24-hours return visits on Days 21,
28, 35, 49 and 63 until the stop criteria are met. This will be followed by 1
follow-up visit to the research center between 5 to 7 days after the last study
day or 24-hours return visit(s).
Day 1 is the day when the volunteer will receive the study compound. The
volunteer is expected at the research center the day before the day of
administration of the study compound and will leave the research center on Day
14 of the study.
Intervention
Only for Part A: 1x 180 mg 14C-leriglitazone will be given as cloudy drink
(oral suspension).
Only for Part B: 1x 180 mg leriglitazone will be given as cloudy drink (oral
suspension). Then after 1.5 hours, 100 µg 14C-leriglitazone will be given as an
intravenous infusion, once during 15 minutes.
Study burden and risks
Blood draw
Drawing blood may be painful or cause some bruising. The use of the indwelling
cannula can sometimes lead to inflammation, swelling, hardening of the vein,
blood clotting, and bleeding in the environment of the puncture site. In some
individuals, a blood draw can sometimes cause pallor, nausea, sweating, low
heart rate, or drop in blood pressure with dizziness or fainting.
In total, we will take about 493 milliliters (mL) blood from participants in
Part A and 469 milliliters (mL) blood from participants in Part B from
screening to follow-up. This amount does not cause any problems in adults. If
the investigator thinks it is necessary for the safety of a participant, extra
samples might be taken for possible additional testing. If this happens, the
total amount of blood drawn may be more than the amount indicated above.
Heart tracing
To make a heart tracing, electrodes will be placed on your arms, chest and
legs. Prolonged use of these electrodes can cause skin irritation.
Coronavirus test
Samples for the coronavirus test will be taken from the back of your nose and
throat using swabs. Taking the samples only takes a few seconds, but can cause
discomfort and can give an unpleasant feeling. Taking a sample from the back of
your throat may cause you to gag. When the sample is taken from the back of
your nose, you may experience a stinging sensation and your eyes may become
watery.
Avenida Ernest Lluch 32, TCM3
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Avenida Ernest Lluch 32, TCM3
MATARÓ (Barcelona) 08302
ES
Listed location countries
Age
Inclusion criteria
1. Sex: male.
2. Age: 18 to 55 years, inclusive, at screening.
3. Body mass index (BMI): 18.0 to 30.0 kg/m2, inclusive, at screening.
4. Status: healthy subjects.
5. Male subjects, if not surgically sterilized, must agree to use adequate
contraception and not donate sperm from admission to the clinical research
center until 90 days after the follow-up visit. Adequate contraception for the
male subject (and his female partner, if she is of childbearing potential) is
defined as using hormonal contraceptives or an intrauterine device combined
with at least 1 of the following forms of contraception: a diaphragm, a
cervical cap, or a condom. Total abstinence, in accordance with the lifestyle
of the subject, is also acceptable.
Further criteria apply.
Exclusion criteria
1. Employee of contract research organization (CRO) or the Sponsor.
2. Evidence of clinically relevant pathology.
3. Known Type 1 or Type 2 diabetes.
4. Previous or current history of cancer (other than treated basal cell
carcinoma).
5. Current suicidal ideation with an intention or plan to act, or a previous
suicide attempt.
Further criteria apply.
Design
Recruitment
Medical products/devices used
Followed up by the following (possibly more current) registration
No registrations found.
Other (possibly less up-to-date) registrations in this register
No registrations found.
In other registers
| Register | ID |
|---|---|
| EudraCT | EUCTR2021-006663-24-NL |
| CCMO | NL80461.056.22 |