Clinical trial NCT02835976: A Study of the Excretion Balance of Radiocarbon and the Pharmacokinetics and Metabolic Profile of TRO19622 (Olesoxime)
Official title: A Single-Center, Open-Label, Single Oral Dose Phase I Study to Determine the Excretion Balance of Radiocarbon (i.e., the Sum of 14C-Labeled TRO19622 and Its 14C-Metabolites) and to Investigate the Pharmacokinetics and Metabolic Profile of TRO19622
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy Volunteer
Lead sponsor: Hoffmann-La Roche
Sponsor class: INDUSTRY
Collaborators: name: Trophos SA
First posted: 2016-07-18
Enrollment: 6
Sex: MALE
Minimum age (years): 55
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: TREATMENT

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.


Eligibility criteria: Inclusion Criteria:

* 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

Exclusion Criteria:

* 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

Primary outcomes:
measure: T1/2 of Radiocarbon
timeFrame: 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
measure: Apparent Plasma Clearance (CL/F) of Olesoxime and Any Major Metabolite(s) Identified
timeFrame: 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
measure: CL/F of Radiocarbon
timeFrame: 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
measure: Apparent Volume of Distribution (Vz/F) of Olesoxime and Any Major Metabolite(s) Identified
timeFrame: 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
measure: Vz/F of Radiocarbon
timeFrame: 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
measure: Cumulative Amount of Olesoxime Excreted in Urine
timeFrame: 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
measure: Cumulative Amount of Olesoxime Excreted in Expired Air
timeFrame: Pre-dose (0 h) and post-dose (8, 10, 12, 16, 24, 48, 72, 96 h) following single dose on Day 1
measure: Cumulative Amount of Olesoxime Excreted in Feces
timeFrame: 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
measure: Renal Clearance (CLr) of Olesoxime
timeFrame: 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
measure: AUClast of Radiocarbon
timeFrame: 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
measure: AUCinf of Radiocarbon
timeFrame: 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
measure: Percentage of Participants with Adverse Events (AEs)
timeFrame: Continuously from Screening until 7 days after last dose (up to 46 days overall)
measure: Maximum Observed Concentration (Cmax) of Olesoxime and Any Major Metabolite(s) Identified
timeFrame: 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
measure: Cmax of Radiocarbon
timeFrame: 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
measure: Time of Maximum Observed Concentration (Tmax) of Olesoxime and Any Major Metabolite(s) Identified
timeFrame: 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
measure: Tmax of Radiocarbon
timeFrame: 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
measure: Area Under the Concentration-Time Curve from Drug Administration to Last Quantifiable Concentration (AUClast) of Olesoxime and Any Major Metabolite(s) Identified
timeFrame: 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
measure: Area Under the Concentration-Time Curve Extrapolated to Infinity (AUCinf) of Olesoxime and Any Major Metabolite(s) Identified
timeFrame: 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
measure: Elimination Half-Life (t1/2) of Olesoxime and Any Major Metabolite(s) Identified
timeFrame: 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
Secondary outcomes:
Other outcomes:
Locations:
Study officials:
affiliation: Hoffmann-La Roche
name: Clinical Trials
role: STUDY_DIRECTOR
References: