An Open-Label, Two-Part Study Designed to Assess the Absolute Bioavailability and Mass Balance of Aramchol

A two-part open-label study to assess the absolute bioavailability of aramchol and the mass balance recovery, metabolite profile and identification of metabolite structures for [14C]-aramchol in healthy male subjects.

A subject was considered evaluable in Part 1 if they provided PK samples for up to a minimum of 120 h after first investigational medicinal product (IMP) administration. A subject was considered evaluable in Part 2 if they provided biological samples for up to a minimum of 144 h after IMP administration or demonstrated >90% mass balance recovery, or <1% of the administered dose eliminated in excreta for 2 consecutive days, whichever was sooner.

Inclusion criteria

• Healthy males
• Aged 35 to 64 years at the time of signing informed consent
• Body mass index (BMI) of 18.0 to 35.0 kg/m2 as measured at screening
• Must be willing and able to communicate and participate in the whole study
• Must have regular bowel movements (ie average stool production of ≥1 and ≤3 stools per day)
• Must provide written informed consent
• Must agree to adhere to the contraception requirements

Exclusion criteria

• Subjects who have received any IMP in a clinical research study within the 90 days prior to Day 1
• Subjects who are study site employees, or immediate family members of a study site or sponsor employee
• History of any drug or alcohol abuse in the past 2 years
• Regular alcohol consumption >21 units per week (1 unit = ½ pint beer, or a 25 mL shot of 40% spirit, 1.5 to 2 Units = 125 mL glass of wine, depending on type)
• A confirmed positive alcohol breath test at screening or each admission
• Current smokers and those who have smoked within the last 12 months. A confirmed breath carbon monoxide reading of greater than 10 ppm at screening or each admission
• Current users of e-cigarettes and nicotine replacement products and those who have used these products within the last 12 months
• Subjects with pregnant or lactating partners
• Radiation exposure, including that from the present study, excluding background radiation but including diagnostic x-rays and other medical exposures, exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years. No occupationally exposed worker, as defined in the Ionising Radiation Regulations 2017, shall participate in the study
• Participation in any study involving administration of any [14C]-labelled compound within 12 months prior to dosing in Part 1 of this study