An Open-label Study of Excretion Balance and Pharmacokinetics Following a Single Oral Dose of [14C]-Venglustat (2.67 MBq) in Healthy Male Subjects

BEX13673

Primary Objectives: * To determine the excretion balance and systemic exposure of radioactivity after oral administration of \[14C\]-venglustat. * To determine the pharmacokinetics (PK) of venglustat and its contribution to the overall exposure of radioactivity. * To determine the metabolic pathways, metabolite profile, chemical structures and main excretion route of the main venglustat metabolites and the metabolite contribution to the overall exposure of radioactivity. Secondary Objective: To assess the clinical and biological tolerability of oral solution of venglustat

2020-05-26

2020-06-26

2020-06-26

Completed

Early phase I

6

Inclusion Criteria: * Body weight between 50.0 and 100.0 kg, inclusive, body Mass Index 18 to 32 kg/m2, inclusive * Certified as healthy by a comprehensive clinical assessment * Normal vital signs after 10 minutes resting in supine position * Standard 12-lead electrocardiogram (ECG) parameters after 10 minutes resting in supine position in the following ranges; 120 ms≤PR≤230 msec, QRS≤120 msec, QTc≤450 msec and normal ECG tracing unless the Investigator considers an ECG tracing abnormality to be not clinically relevant * Laboratory parameters within the normal range * Having given written informed consent prior to undertaking any study-related procedure * Covered by a health insurance system where applicable, and/or in compliance with the recommendations of the national laws in force relating to biomedical research * Not under any administrative or legal supervision * Normal renal function as expressed by a creatinine clearance \>80 mL/min as calculated by the Cockroft and Gault formula * Male subjects who agree to use condoms, whose female partner(s) are of childbearing potential (including lactating women), must accept to use, during sexual intercourse, a double contraception method (unless they underwent surgical sterilization) until 90 days after the end of study Exclusion Criteria: * Any history or presence of clinically relevant cardiovascular, pulmonary, gastrointestinal, hepatic, renal, metabolic, hematological, neurological, osteomuscular, articular, psychiatric, systemic, ocular, or infectious disease, or signs of acute illness * Frequent headaches and/or migraine, recurrent nausea and/or vomiting (for vomiting only: more than twice a month). * Blood donation, any volume, within 3 months before inclusion. * Symptomatic postural hypotension, irrespective of the decrease in blood pressure. * Presence or history of clinically significant drug hypersensitivity, or allergic disease diagnosed and treated by a physician that in the opinion of the Investigator would compromise subject safety. * History or presence of drug or alcohol abuse (alcohol consumption more than 14 units per week on a regular basis) in the 5 years prior to screening. * Smoking or using nicotine replacement products or e-cigarettes regularly more than 5 cigarettes or equivalent per week, unable to stop smoking during the study (occasional smoker can be enrolled). * Excessive consumption of beverages containing xanthine bases (more than 4 cups or glasses per day) * Any medication (including St John's Wort) within 14 days before inclusion or within 5 times the elimination half-life or pharmacodynamic half-life of the medication; any vaccination or any medications known to be CYP3A4 inducers within the last 28 days and any biologics (antibody or its derivatives) given within 4 months before inclusion * Subjects who do not have suitable veins for multiple venepunctures/cannulation as assessed by the Investigator at screening. * Any subject who, in the judgment of the Investigator, is likely to be noncompliant during the study, or unable to cooperate because of a language problem or poor mental development. * Any subject enrolled in or having participated, in \[this or\] any other clinical study involving an investigational medicinal product (IMP) according to applicable regulations/guidelines in the 3 months prior to dosing of this study. * Any subject who cannot be contacted in case of emergency. * Any subject who is the Investigator or any sub investigator, research assistant, pharmacist, study coordinator, or other staff thereof, directly involved in conducting the study * Positive result on any of the following tests: hepatitis B surface (HBs Ag) antigen, anti-hepatitis C virus (anti-HCV) antibodies, anti-human immunodeficiency virus 1 and 2 antibodies (anti-HIV1 and anti HIV2 Ab). * Confirmed positive result on urine drug screen (amphetamines/methamphetamines, barbiturates, benzodiazepines, cannabinoids, cocaine, tricyclic antidepressants, opiates including methadone). * Positive alcohol breath test * Any subject with specific dietary habits, such as vegan. * Any subject with irregular bowel habits (more than 3 bowel movements/day or less than 1 every 2 days). * Any subject undergoing dental care or presenting with dental caries. * Any subject who is occupationally exposed to radiation as defined in the Ionizing Radiations Regulations 2017 * Participation in a trial with 14C-radiolabelled medication in the 12 months preceding the study. * Radiation exposure, including that from the present study and radiopharmaceuticals or radionuclides in therapeutic or diagnostic procedures, but excluding background radiation, exceeding 5 millisievert (mSv) in the last 12 months or 10 mSv in the last 5 years. * Any consumption of citrus (grapefruit, orange, etc) or their juices within 5 days before inclusion The above information is not intended to contain all considerations relevant to a potential participation in a clinical trial.

{'studyType': 'INTERVENTIONAL', 'phases': ['PHASE1'], 'designInfo': {'allocation': 'NA', 'interventionModel': 'SINGLE_GROUP', 'primaryPurpose': 'SCREENING', 'maskingInfo': {'masking': 'NONE'}}, 'enrollmentInfo': {'count': 6, 'type': 'ACTUAL'}}

2023-09-26