Mass Balance Recovery and Metabolic Profile of 14C Debio 1450 Following Single Oral and Intravenous Doses in Healthy Male Subjects

A Phase I, Two-part, Open-label, Non-randomised Study to Investigate the Mass Balance Recovery and Metabolic Profile of 14C Debio 1450 Following Single Oral and Intravenous Doses in Healthy Male Subjects

The primary objectives of this study are:

• To determine the mass balance recovery (expired air, urine and faeces) and route and rate of elimination of 14C-Debio 1450.
• To determine the metabolic profile of 14C-Debio 1450 in whole blood, plasma, urine and faeces.
• To determine the pharmacokinetics of total radioactivity and of Debio 1450 (prodrug) and Debio 1452 (active moiety) in plasma and urine.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: [14C-pos 1]-Debio 1450 BES Solution; Drug: [14C-pos 25]-Debio 1450 BES Solution

• Study Type: Interventional
• Enrollment (Actual): 18
• Phase: Phase 1

Contacts and Locations

Study Locations

• United Kingdom
  • Leeds, United Kingdom, LS2 9LH
    • Covance Clinical Research Unit (CRU) Ltd.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 35 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Meets protocol-specified criteria for qualification and contraception
• Is willing and able to remain confined in the study unit for the entire duration of each treatment period and comply with restrictions related to food, drink and medications
• Voluntarily consents to participate and provides written informed consent prior to any protocol-specific procedures

Exclusion Criteria:

• Has history or current use of over-the-counter medications, dietary supplements, or drugs (including nicotine and alcohol) outside protocol-specified parameters

• Has signs, symptoms or history of any condition that, per protocol or in the opinion of the investigator, might compromise:

  1. the safety or well-being of the participant or study staff
  2. the safety or well-being of the participant's offspring (such as through pregnancy or breast-feeding)
  3. the analysis of results

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Non-Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Part A: Cohort 1; Participants receive a single intravenous (IV) dose of 240 mg/3.7 megabecquerel (MBq) of [14C-pos 1]-Debio 1450 BES solution.	Drug: [14C-pos 1]-Debio 1450 BES Solution; A solution containing Debio 1450 bis ethanolamine salt (BES) radiolabelled with carbon-14 (14C) at position 1
Experimental: Part A: Cohort 2; Participants receive a single oral dose of 240 mg/3.7 MBq of [14C-pos 1]-Debio 1450 BES solution.	Drug: [14C-pos 1]-Debio 1450 BES Solution; A solution containing Debio 1450 bis ethanolamine salt (BES) radiolabelled with carbon-14 (14C) at position 1
Experimental: Part B: Cohort 3; Participants receive a single oral dose of 240 mg Debio 1450/37 kilobecquerel (kBq) of [14C-pos 25]-Debio 1450 BES solution.	Drug: [14C-pos 25]-Debio 1450 BES Solution; A solution containing Debio 1450 BES radiolabelled with carbon-14 (14C) at position 25

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Mass balance recovery after a single dose of radiolabelled Debio 1450 measured through total radioactivity excreted in expired air, urine and faeces		168 hours after dosing (Day 8)
Routes of metabolism and excretion after a single dose of radiolabelled Debio 1450 measured through total radioactivity concentrations in expired air, urine and fecaes		168 hours after dosing (Day 8)
Whole blood and plasma partitioning of total radioactivity after a single dose of radiolabelled Debio 1450 through measurement of total radioactivity levels in blood	Blood is collected within the 168 hours as follows: IV infusion: Predose, 1, 1.85, 2.25, 2.5, 3, 4, 5, 8, 14, 18, 24, 36, 48, 60, 72, 96, 120, 144 and 168 hours after the infusion start time; Oral administration: Predose,15 and 30 minutes, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 16, 24, 36, 48, 60, 72, 96, 120, 144 and 168 hours following the oral dose	168 hours after dosing (Day 8)
Percentage of participants with clinically significant change from baseline in vital signs, electrocardiogram, and/or laboratory parameters		168 hours after dosing (Day 8)

Collaborators and Investigators

• Sponsor: Debiopharm International SA
• Investigators: Study Director: Annick Ménétrey, Debiopharm International, S.A.

Study record dates

Study Major Dates

• Study Start: November 1, 2015
• Primary Completion (Actual): December 1, 2015
• Study Completion (Actual): December 1, 2015

Study Registration Dates

• First Submitted: November 2, 2015
• First Submitted That Met QC Criteria: November 2, 2015
• First Posted (Estimate): November 3, 2015

Study Record Updates

• Last Update Posted (Estimate): January 18, 2016
• Last Update Submitted That Met QC Criteria: January 14, 2016
• Last Verified: January 1, 2016

More Information

Terms related to this study

• Keywords: Bioavailability
• Additional Relevant MeSH Terms: Pharmaceutical Solutions
• Other Study ID Numbers: Debio 1450-105; 2015-002604-87 (EudraCT Number)