fibrosis fibrosis inflammatory and fibrosis-related diseases
Conditions
Interventions
[14C]-PBI-4050
Sponsors
Prometic
Eligibility
Age
18 Years to 99 Years
Inclusion criteria
Inclusion criteria: The following criteria must be met by all subjects considered for study participation: 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 21 to 55 years (inclusive) at Screening. 4. A body weight of *60 kg and a body mass index ranging from 18 to 30 kg/m2 at Screening. 5. The subject must agree to minimize the risk of a female partner becoming pregnant from the dosing day until 3 months after the completion of the study. Acceptable methods of contraception for male volunteers include a vasectomy no less than 6 months prior to dosing, barrier contraception or a medically accepted contraceptive method. For female partners of male volunteers, acceptable methods of contraception include intra-uterine device, tubal ligation, hormonal contraceptive since at least two months and diaphragm with spermicide. 6. In the Investigator*s opinion, subject is able to understand the nature of the study and any risks involved in participation, and willing to cooperate and comply with the protocol restrictions and requirements.
Exclusion criteria
Exclusion criteria: Subjects will be excluded if they meet any of the following 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 gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders. 3. History of any major surgery within the last four weeks before participation in this study or any bone fracture within the last two months. 4. Diseases of the central nervous system (such as epilepsy) or psychiatric disorders. 5. Chronic or relevant acute infections. 6. History of allergy/ hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator. 7. History of any bleeding disorder including prolonged or habitual bleeding, other hematologic disease or cerebral bleeding (e.g. after a car accident) or commotion cerebri. 8. Intake of drugs with a long half-life (>24 hours) within 1 month prior to study drug administration. 9. Use of any kind of prescription medication from 14 days prior to the administration of the study drug. 10. Use of over-the-counter products and/or natural health products (including food supplements, herbal supplements, etc.). 11. Participation in another trial with an investigational drug within 2 months prior to administration of the study drug or during the trial. 12. The subject is a smoker (>10 cigarettes or 3 cigars or 3 pipes/day) or uses other nicotine-containing products (for example, snuff, nicotine patches, nicotine chewing gum, mock cigarettes) or is unable to reform from smoking on study days. Ex-smokers must have ceased smoking *3 months prior to Screening. 13. Alcohol abuse (>60 g/day (6 units/day)). 14. History of drug abuse. 15. Blood donation within 3 months prior to administration or during the trial. 16. Any laboratory value outside the reference range, unless considered to lack clinical reference.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| [14C]-radioactivity in plasma and whole blood (C blood cells/C plasma ratio of [14C]-radioactivity). [14C]-radioactivity in urine. Measurement of the plasma protein binding of total [14C]-radioactivity in human plasma samples ex vivo. Maximum observed concentration of the analyte in plasma (Cmax). Plasma concentration-time profiles of total radioactivity in whole blood and plasma. [14C]-metabolic profile and identification of metabolites in urine. [14C]-radioactivity in feces. [14C]-metabolic profile and identification of metabolites in feces. [14C]-metabolic profile and identification of metabolites in plasma. Time from dosing to peak plasma concentration (tmax). Terminal half-life of the analyte in plasma (t1/2). Terminal rate constant of the analyte in plasma (*z). Area under the concentration-time curve of the analyte in plasma from time zero to 24 hours (AUC0-24). Area under the concentration-time curve of the analyte in plasma from time zero to the time of the last quantifiable drug concentration (AUC0-tz). Area under the concentration-time curve of the analyte in plasma from time zero to infinity (AUC0-*). Mean residence time of the analyte molecules in the body after oral administration (MRTpo). Total clearance of the analyte in plasma following extravascular administration (CL/F). Apparent volume of distribution during the terminal phase *z following extravascular administration (Vz/F). Fraction of analyte eliminated in urine from 0 to the limit of the last quantifiable data point (feurine,0-tz). Fraction of analyte eliminated in feces from 0 to the limit of the last quantifiable data point (fefeces,0-tz). Amount of analyte that was eliminated in urine from 0 to the limit of the last quantifiable data point (Aeurine,0-tz). Amount of analyte that was eliminated in feces from 0 to the limit of the last quantifiable data point (Aefeces,0-tz). | — |
Secondary
| Measure | Time frame |
|---|---|
| Change from baseline in vital signs (Day 14 after study drug administration). Change from baseline in clinical laboratory parameters (Day 14 after study drug administration). Number of subjects with adverse events (AEs). Change from baseline in 12-lead ECG (Day 14 after study drug administration). | — |
Countries
Netherlands
Outcome results
None listed