A Study of the Excretion Balance of Radiocarbon and the Pharmacokinetics and Metabolic Profile of TRO19622 (Olesoxime)

NCT02835976 | Completed Phase 1

• 2 other identifiers: WP298672014-002470-37
• Study Type: interventional
• Target: 6
• Locations: 0 countries
• Sites: N/A

Brief Summary

This Phase I study is designed to determine the excretion balance of radiocarbon, as the sum of carbon-14 (14C)-labeled TRO19622 and its 14C-metabolites, and to investigate the pharmacokinetics and metabolic profile of TRO19622 (olesoxime) in healthy participants.

Conditions

Healthy Volunteer

Outcome Measures

Primary Outcomes (19)

• T1/2 of Radiocarbon

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 168, 216, 264, 312, 360, 408 h) following single dose on Day 1

• Apparent Plasma Clearance (CL/F) of Olesoxime and Any Major Metabolite(s) Identified

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360, 384, 408 h) following single dose on Day 1

• CL/F of Radiocarbon

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 168, 216, 264, 312, 360, 408 h) following single dose on Day 1

• Apparent Volume of Distribution (Vz/F) of Olesoxime and Any Major Metabolite(s) Identified

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360, 384, 408 h) following single dose on Day 1

• Vz/F of Radiocarbon

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 168, 216, 264, 312, 360, 408 h) following single dose on Day 1

• Cumulative Amount of Olesoxime Excreted in Urine

  Continuous urine collection from pre-dose (0 h) to post-dose (432 h, or until release criteria are met) following single dose on Day 1

• Cumulative Amount of Olesoxime Excreted in Expired Air

  Pre-dose (0 h) and post-dose (8, 10, 12, 16, 24, 48, 72, 96 h) following single dose on Day 1

• Cumulative Amount of Olesoxime Excreted in Feces

  Continuous fecal collection from pre-dose (0 h) to post-dose (432 h, or until release criteria are met) following single dose on Day 1

• Renal Clearance (CLr) of Olesoxime

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360, 384, 408 h) following single dose on Day 1

• AUClast of Radiocarbon

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 168, 216, 264, 312, 360, 408 h) following single dose on Day 1

• AUCinf of Radiocarbon

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 168, 216, 264, 312, 360, 408 h) following single dose on Day 1

• Percentage of Participants with Adverse Events (AEs)

  Continuously from Screening until 7 days after last dose (up to 46 days overall)

• Maximum Observed Concentration (Cmax) of Olesoxime and Any Major Metabolite(s) Identified

  Pre-dose (0 hours [h]) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360, 384, 408 h) following single dose on Day 1

• Cmax of Radiocarbon

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 168, 216, 264, 312, 360, 408 h) following single dose on Day 1

• Time of Maximum Observed Concentration (Tmax) of Olesoxime and Any Major Metabolite(s) Identified

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360, 384, 408 h) following single dose on Day 1

• Tmax of Radiocarbon

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 168, 216, 264, 312, 360, 408 h) following single dose on Day 1

• Area Under the Concentration-Time Curve from Drug Administration to Last Quantifiable Concentration (AUClast) of Olesoxime and Any Major Metabolite(s) Identified

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360, 384, 408 h) following single dose on Day 1

• Area Under the Concentration-Time Curve Extrapolated to Infinity (AUCinf) of Olesoxime and Any Major Metabolite(s) Identified

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360, 384, 408 h) following single dose on Day 1

• Elimination Half-Life (t1/2) of Olesoxime and Any Major Metabolite(s) Identified

  Pre-dose (0 h) and post-dose (2, 4, 6, 8, 10, 12, 16, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, 336, 360, 384, 408 h) following single dose on Day 1

Study Arms (1)

Olesoxime

EXPERIMENTAL

Participants will receive a single dose of liquid suspension of 14C-labeled olesoxime containing an equivalent of 600 milligrams (mg) of the compound. The total amount of administered radiocarbon will be 93 microcuries (mcCi), or 3.447 megabecquerels (MBq).

Drug: Olesoxime

Interventions

Olesoxime DRUG

Olesoxime will be given orally on Day 1 as a 600-mg liquid suspension within 30 minutes after starting a standardized high-fat breakfast.

Also known as: TRO19622

Olesoxime

Eligibility Criteria

• Age: 55 Years - 65 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Body mass index (BMI) 20.0 to 28.0 kilograms per meter-squared (kg/m\^2) and body weight at least 60 kilograms (kg)
• Fitzpatrick skin type less than (\<) 4
• Good health according to medical history, physical examination, laboratory parameters, vital signs, and 12-lead electrocardiogram (ECG)
• Negative urine test for drugs of abuse
• Negative alcohol breath test
• Negative tests for hepatitis or human immunodeficiency virus (HIV)
• Use of effective contraception during and for 3 months beyond study participant, among sexually active non-vasectomized participants with females partners of childbearing potential

You may not qualify if:

• Concomitant or recent medication use within 2 weeks prior to Day 1, except for paracetamol
• Use of enzyme-inducing drugs within 2 months prior to Day 1
• Any medical condition that may alter the pharmacokinetics of olesoxime or affect interpretation of study results
• Irregular bowel movements
• Drug addiction or alcoholism
• Use of nicotine products
• Participation in another clinical study within 12 weeks prior to Day 1
• Exposure to ionizing radiation within one year prior to Day 1

Sponsors & Collaborators

• Hoffmann-La Roche: lead
• Trophos SA: collaborator

MeSH Terms

Interventions

olesoxime

Study Officials

• Clinical Trials

  Hoffmann-La Roche

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 14, 2016
• First Posted: July 18, 2016
• Study Start: July 1, 2014
• Primary Completion: September 1, 2014
• Study Completion: September 1, 2014
• Last Updated: July 18, 2016

Record last verified: 2016-07