Primary objectives:To determine the ratio of parent drug to metabolites in the circulation following administration of a single oral dose of 400 mg [14C]-EYP001a containing 100 µCi radioactivity.Profiling of EYP001a metabolites in blood, urine and…
ID
Source
Brief title
Condition
- Other condition
Synonym
Health condition
Chronic liver diseases, HBV/NASH
Research involving
Sponsors and support
Intervention
Outcome measures
Primary outcome
The following parameters will be calculated, whenever possible and appropriate
and taking into account the last time point where detectable radioactivity
counts were observed:
Radioactivity-time profiles in whole blood and plasma.
Maximum observed total radioactivity in plasma and whole blood (Cmax).
Time from dosing to peak total radioactivity in plasma and whole blood (tmax).
Area under the total radioactivity-time curve in plasma and whole blood from
time zero to 24 hours (AUC0-24).
Area under the total radioactivity-time curve in plasma and whole blood from
time zero to the time of the last quantifiable drug concentration (AUC0-tz).
Area under the total radioactivity-time curve in plasma and whole blood from
time zero to infinity (AUC0-inf).
[14C]-metabolic profile and identification of metabolites in plasma.
[14C]-radioactivity in urine.
[14C]-metabolic profile and identification of metabolites in urine.
[14C]-radioactivity in feces.
[14C]-metabolic profile and identification of metabolites in feces.
Secondary outcome
Vital signs values;
Clinical laboratory values;
Number of subjects with adverse events (AEs);
12-lead ECG values.
Background summary
ENYO Pharma is developing EYP001a, a selective synthetic, non-bile salt,
carboxylic acid farnesoid X receptor (FXR) agonist, for the treatment of
chronic hepatitis B virus (HBV) infection and non-alcoholic steatohepatitis
(NASH). Chronic liver diseases are major public health problems [1]. Current,
but probably undervalued, worldwide estimations show that 844 million people
have chronic liver diseases, with a mortality rate of 2 million deaths per
year. While viral chronic liver diseases such as HBV infection are predominant
in Asia, Africa and Latin America, emergent metabolic diseases (i.e.,
non-alcoholic fatty liver disease (NAFLD), and NASH) are the most common causes
of chronic liver diseases in Western countries. Patients with NASH and chronic
HBV infection have increased rates of liver-related mortality due to the
development of complications, including fibrosis, cirrhosis, and hepatocellular
carcinoma (HCC). There is therefore an urgent need for improved treatment
options for both chronic liver diseases.
Study objective
Primary objectives:
To determine the ratio of parent drug to metabolites in the circulation
following administration of a single oral dose of 400 mg [14C]-EYP001a
containing 100 µCi radioactivity.
Profiling of EYP001a metabolites in blood, urine and feces.
To determine the mass balance of drug-related materials following
administration of a single oral dose of 400 mg [14C]-EYP001a containing 100 µCi
radioactivity.
To determine the primary route of excretion of drug-related materials following
administration of a single oral dose of 400 mg [14C]-EYP001a containing 100 µCi
radioactivity.
To determine the total radioactivity versus time profile in plasma and whole
blood following administration of a single oral dose of 400 mg [14C]-EYP001a
containing 100 µCi radioactivity.
Secondary objective:
To investigate the safety and tolerability of a single oral dose of 400 mg
[14C]-EYP001a containing 100 µCi radioactivity in healthy subjects.
Study design
The present study is designed to investigate the absorption, metabolism,
excretion as well as safety/tolerability of EYP0001a following
the administration of a single oral dose to healthy male volunteers.
Intervention
[14C]-ENP001a, single dose
Study burden and risks
Since this study is being executed in healthy volunteers, there are no
anticipated benefits of the IMP. Please see the IMPD for further
information.
Bâtiment Domilyon 321 Avenue Jean Jaurès
Lyon 69007
FR
Bâtiment Domilyon 321 Avenue Jean Jaurès
Lyon 69007
FR
Listed location countries
Age
Inclusion criteria
1. Able to provide informed consent to participate in this study after reading
the participant information sheet and informed consent form and after having
the opportunity to discuss the study with the Investigator or designee.
2. Healthy and free from clinically significant illness or disease as
determined by medical history, physical examination, laboratory and other tests
at Screening.
3. Male Caucasian subjects, aged 18 to 60 years (inclusive) at Screening.
Exclusion criteria
1. Any finding of the medical examination (including blood pressure, pulse rate
and ECG) deviating from normal and of clinical relevance.
2. History or current clinically significant gastrointestinal, hepatic, renal,
respiratory, cardiovascular, metabolic, immunologic, hormonal disorders.
3. History of any major surgery within the last 4 weeks before participation in
this study or any bone fracture within the last 2 months.
Design
Recruitment
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 | EUCTR2019-001304-37-NL |
| CCMO | NL70237.056.19 |