Single Dose ADME Study of [14C]-Rencofilstat in Healthy Male Subjects
Study Details
Study Description
Brief Summary
This is a single-center, single-period, single-dose, open-label, non-randomized study to assess the mass balance recovery, metabolite profile and metabolite identification of 14C- labelled rencofilstat ([14C] CRV431). It is planned to enroll 6 healthy male subjects in a single group. Each subject will receive a single 225 mg oral dose of [14C] CRV431 self-micro emulsifying drug delivery system (SMEDDS) oral emulsion.
| Condition or Disease | Intervention/Treatment | Phase |
|---|---|---|
|
Early Phase 1 |
Detailed Description
This is a single center, open-label, non-randomized, single period, single dose study in healthy male subjects designed to assess the mass balance recovery, pharmacokinetics (PK), metabolite profile and metabolite identification of rencofilstat. It is planned to enroll a single cohort of 6 subjects. All subjects will receive a single 225 mg oral dose of [14C]-rencofilstat, as a SMEDDS oral emulsion in the fasted state.
Subjects will undergo preliminary screening procedures for the study at the screening visit (Day -28 to Day -2). Subjects will be admitted in the evening on the day before dosing (Day-1).
Whole blood, plasma, urine and feces samples will be collected at regular intervals for PK analysis, total radioactivity analysis, metabolite profiling, mass balance and safety as applicable, from pre-dose to discharge from the clinical unit. Urine and feces samples may be collected at return visits or home visits if mass balance criteria have not been met by a subject.
Study Design
Arms and Interventions
| Arm | Intervention/Treatment |
|---|---|
| Experimental: [14C]-RCF 225mg [14C]-rencofilstat, 225mg oral dose, self-micro-emulsifying drug delivery system, single dose |
Drug: [14C]-rencofilstat 225mg
radio-labelled 225mg oral dose of rencofilstat
Other Names:
|
Outcome Measures
Primary Outcome Measures
- To determine the mass balance recovery after a single oral dose of [14C]-rencofilstat [22 Days]
Cumulative amount of total radioactivity recovered.
Eligibility Criteria
Criteria
Inclusion Criteria:
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Healthy males
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Aged 30 to 65 years inclusive at the time of signing informed consent
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Body mass index (BMI) of 18.0 to 35.0 kg/m2 as measured at screening
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Must be willing and able to communicate and participate in the whole study
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Must have regular bowel movements (ie average stool production of ≥1 and ≤3 stools per day)
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Must provide written informed consent
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Must agree to adhere to the contraception requirements
Exclusion Criteria:
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Subjects who have received any investigational treatment in a clinical research study within the 90 days prior to Day 1, or less than 5 elimination half-lives prior to Day 1, whichever is longer
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Subjects who are, or are immediate family members of, a study site or sponsor employee
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Evidence or history of current SARS-CoV-2 infection within 4 weeks prior to study drug administration
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History of any drug or alcohol abuse in the past 2 years prior to screening
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Regular alcohol consumption in males >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)
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A confirmed positive alcohol breath test at screening or admission
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Current smokers and those who have smoked within the last 12 months prior to screening
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A confirmed breath carbon monoxide reading of greater than 10 ppm at screening or admission
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Current users of e-cigarettes and nicotine replacement products and those who have used these products within the last 12 months prior to screening
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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
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Subjects who do not have suitable veins for multiple venipunctures/cannulation as assessed by the investigator or delegate at screening
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Clinically significant abnormal clinical chemistry, haematology or urinalysis as judged by the investigator. Subjects known to have Gilbert's syndrome are excluded
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Confirmed positive drugs of abuse test result
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Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) antibody results
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Evidence of renal impairment at screening, as indicated by an estimated eGFR of <60 mL/min/1.73m2 using the Chronic Kidney Disease Epidemiology Collaboration equation
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History of clinically significant cardiovascular, renal, hepatic, dermatological, chronic respiratory or gastrointestinal disease, malabsorptive, neurological or psychiatric disorder, as judged by the investigator
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Serious adverse reaction or serious hypersensitivity to any drug or the formulation excipients
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Presence or history of clinically significant allergy requiring treatment, as judged by the investigator. Hay fever is allowed unless it is active
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Donation of blood or plasma within the previous 3 months or loss of greater than 400 mL of blood
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Subjects who have taken known strong or moderate CYP3A4 inducers in the 30 days before IMP administration
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Subjects who are taking, or have taken, any prescribed or over-the-counter drug or herbal remedies (other than up to 4 g of paracetamol per day) in the 14 days before study drug administration. Exceptions may apply, as determined by the investigator, if each of the following criteria are met: medication with a short half-life if the washout is such that no pharmacodynamic activity is expected by the time of dosing with study drug; and if the use of medication does not jeopardize the safety of the trial subject; and if the use of medication is not considered to interfere with the objectives of the study
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Subjects who have had a COVID-19 vaccine 7 days before dosing
Contacts and Locations
Locations
No locations specified.Sponsors and Collaborators
- Hepion Pharmaceuticals, Inc.
Investigators
- Principal Investigator: Litza McKenzie, MD, Quotient Sciences
Study Documents (Full-Text)
None provided.More Information
Publications
None provided.- HEPA-CRV431-105