An Open Label, Single-dose, Single-period Study Designed to Assess the Mass Balance Recovery, Metabolite Profile and Metabolite Identification of [14C]-Pracinostat in Healthy Male Subjects
Overview
- Phase
- Phase 1
- Intervention
- pracinostat
- Conditions
- Healthy Subjects
- Sponsor
- Helsinn Healthcare SA
- Enrollment
- 6
- Locations
- 1
- Primary Endpoint
- mass balance recovery
- Status
- Completed
- Last Updated
- 6 years ago
Overview
Brief Summary
The current study is designed to generate data for the investigation of absorption, distribution, metabolism and elimination (ADME) processes of pracinostat in humans, as well as generating samples for metabolite profiling and structural identification. The mass balance recovery of pracinostat following administration of [14C]-pracinostat will be assessed, as well as metabolite profiling and identification of pracinostat in healthy male subjects. In addition, this study will provide further PK and safety data in healthy subjects.
Investigators
Eligibility Criteria
Inclusion Criteria
- •Healthy males
- •Age 40 to 65 years, inclusive
- •Body mass index of 18.0 to 35.0 kg/m2 or, if outside the range, considered not clinically significant by the investigator
- •Must be willing and able to communicate and participate in the whole study
- •Must have regular bowel movements (i.e., average stool production of ≥1 and ≤3 stools per day)
- •Subject is considered healthy on the basis of medical history, physical examination, triplicate electrocardiogram (ECG), vital signs and clinical laboratory assessments.
- •Provision of written informed consent to participate as shown by a signature on the volunteer consent form.
- •Male subjects must not be seeking to father a child in the next 6 months (covering 2 cycles of spermatogenesis) and must agree to use an adequate method of contraception -
Exclusion Criteria
- •Subjects who have received any IMP in a clinical research study within the previous 3 months
- •Subjects who are study site employees, or immediate family members of a study site or sponsor employee
- •Subjects with pregnant partners
- •Subjects who have previously been enrolled in this study
- •Subjects who have been enrolled in an absorption, distribution, metabolism and elimination (ADME) study in the last 12 months
- •History of any drug or alcohol abuse in the past 2 years
- •Regular alcohol consumption in males \>21 units per week (1 unit = ½ pint beer, 25 mL of 40% spirit; 1.5 to 2 units = 125 mL glass of wine, depending on type)
- •Current smokers and those who have smoked within the last 12 months. A positive urine cotinine test at screening and admission
- •Current users of e-cigarettes and nicotine replacement products and those who have used these products within the last 12 months
- •Radiation exposure, excluding background radiation but including significant medical exposures, or other trial related exposures, in the 12 months preceding participation in the trial, or radiation exposure exceeding 10 mSv in the 5 years preceding participation in the trial, inclusive of the 5 mSv exposure resulting from participation in this study. No occupationally exposed worker, as defined in the Ionising Radiation Regulations 1999, shall participate in the study. Significance of a medical exposure will be determined by the investigator.
Arms & Interventions
single oral administration of 14C-pracinostat in the fas
Intervention: pracinostat
Outcomes
Primary Outcomes
mass balance recovery
Time Frame: up to 12 days
urine and faeces will becollected at different time points and the radioactivity will be measured. The recovery will be expressed as percentage of radioactivity administrated
Area Under the Curve (AUC)
Time Frame: up to 8 days
blood and plasma samples will be collected and the radioactivity measured to determine the Area under the concentration-time curve
Maximum concentration (Cmax)
Time Frame: up to 8 days
blood and plasma samples will be collected and the radioactivity measured to determine the max concentration in concentration-time curve
clearance (CL/F)
Time Frame: up to 8 days
systemic clearance after extravascular administration
Volume of distribution (Vd/F)
Time Frame: up to measurable concentration
volume of distribution after extravascular administration
terminal half life (t1/2)
Time Frame: up to 8 days
blood and plasma samples will be collected and the radioactivity measured to determine the terminal half life of the concentration-time curve