Study Evaluating Pharmacokinetics and Mass Balance of [14C]-CTP-543 in Healthy Adult Male Volunteers

A Phase 1, Open-label Study to Assess the Absorption, Metabolism, Excretion, and Mass Balance of Oral [14C]-CTP-543 in Healthy Adult Male Subjects

This study will assess the absorption, metabolism, excretion, mass balance, safety, and tolerability of a single oral administration of [14C]-CTP-543 in healthy male subjects.

Study Overview

• Status: Completed
• Conditions: Healthy Volunteers
• Intervention / Treatment: Drug: [14C]-CTP-543

• Study Type: Interventional
• Enrollment (Actual): 6
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Nebraska
    • Lincoln, Nebraska, United States, 68502
      • Celerion

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 19 years to 55 years (ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Healthy male subjects between the ages of 19 and 55 years, inclusive (healthy is determined by medical evaluation, including medical history, full physical examination, vital signs, electrocardiogram, and clinical laboratory tests)
• Body Mass Index of 18.0 to 32.0 kg/m2
• Continuous non smoker who has not used nicotine containing products for at least 3 months prior to dosing and throughout the study

Exclusion Criteria:

• Known immunodeficiency disorder, including positive serology for human immunodeficiency virus (HIV) at screening
• Infection with hepatitis B or hepatitis C viruses
• History of irregular bowel movements
• History of herpes zoster
• A positive tuberculosis test at screening or history of incompletely treated or untreated tuberculosis
• History or presence of alcoholism or drug abuse within the past 2 years prior to dosing
• Participation in another clinical study within 30 days prior to dosing

Study Plan

How is the study designed?

Design Details

• Primary Purpose: BASIC_SCIENCE
• Allocation: NA
• Interventional Model: SINGLE_GROUP
• Masking: NONE

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: Investigational Product; [14C]-CTP-543	Drug: [14C]-CTP-543; Single dose of radiolabeled CTP-543 (approximately 75 μCi) administered as an oral solution

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Mass balance: Calculation of percent of total radioactivity recovered in urine		From time zero up to 96 hours post-dose following oral administration of [14C]-CTP-543 up to Day 15
Mass balance: Calculation of percent of total radioactivity recovered in feces		From time zero up to 96 hours post-dose following oral administration of [14C]-CTP-543 up to Day 15
CTP-543 PK: Cmax	Maximum plasma concentration	Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
CTP-543 PK: Tmax	Time for Cmax	Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
CTP-543 PK: t1/2		Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
CTP-543 PK: AUClast	Area under the plasma concentration time profile from time 0 to time of the last quantifiable concentration (Clast)	Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
CTP-543 PK: AUCinf	Area under the plasma concentration time profile from time 0 to infinity	Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
CTP-543 PK: CL/F	Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood (rate at which a drug is metabolized or eliminated by normal biological processes).	Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
CTP-543 PK: Vz/F	Apparent volume of distribution following oral administration	Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
CTP-543 metabolite PK: Cmax	Maximum plasma concentration	Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
CTP-543 metabolite PK: Tmax	Time for Cmax	Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
CTP-543 metabolite PK: t1/2		Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
CTP-543 metabolite PK: AUC0-last	Area under the plasma concentration time profile from time 0 to time of the last quantifiable concentration (Clast)	Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
CTP-543 metabolite PK: AUCinf	Area under the plasma concentration time profile from time 0 to infinity	Pre-dose, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 96 hours post-dose
Total [14C]: urine	Total radioactivity excreted into the urine from time zero to the time of last measurable concentration following oral administration of [14C]-CTP-543	Pre-dose up to 336 hours post-dose
Total [14C]: feces	Total radioactivity excreted into the feces from time zero to the time of last measurable concentration following oral administration of [14C]-CTP-543	Pre-dose up to 336 hours post-dose
Total radioactivity in whole blood		Pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96 hours post-dose
Total radioactivity in plasma		Pre-dose, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, 36, 48, 72, 96 hours post-dose

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Adverse events	Number of adverse events, which are any untoward medical occurrence regardless of attribution to study drug in a participant who received study drug	Screening up to Day 15
Number of Participants With Clinically Significant Change From Baseline in Heart Rate	Heart rate measured in beats per minute (bpm)	Screening, Pre-dose, 2, 8, 48 hours post-dose
Number of Participants With Clinically Significant Change From Baseline in Blood Pressure	Blood pressure measured in millimeters of mercury (mmHg)	Screening, Pre-dose, 2, 8, 48 hours post-dose
Number of Participants With Clinically Significant Change From Baseline in Respiratory Rate	Respiratory rate measured in breaths per minute	Screening, Pre-dose, 2, 8, 48 hours post-dose
Number of Participants With Clinically Significant Change From Baseline in Temperature	Temperature measured in Celsius (°C)	Screening, Pre-dose, 2, 8, 48 hours post-dose
Number of Participants With Clinically Significant Change From Baseline in Hematology		Screening, Check-in, 8, 24 hours postdose
Number of Participants With Clinically Significant Change From Baseline in Serum Chemistry		Screening, Check-in, 8, 24 hours postdose
Number of Participants With Clinically Significant Change From Baseline in Coagulation		Screening, Check-in, 8, 24 hours postdose
Number of Participants With Clinically Significant Change From Baseline in Urinalysis		Screening, Check-in, 8, 24 hours postdose
Number of Participants With Clinically Significant Changes to the Physical Examination	Clinically significant changes to the physical examination	Screening up to Day 15
Number of Participants With Clinically Significant Change From Baseline in Electrocardiogram - P Wave		Screening, Pre-dose, 48 hours post-dose
Number of Participants With Clinically Significant Change From Baseline in Electrocardiogram - QRS Complex		Screening, Pre-dose, 48 hours post-dose
Number of Participants With Clinically Significant Change From Baseline in Electrocardiogram - QT Interval		Screening, Pre-dose, 48 hours post-dose

Collaborators and Investigators

• Sponsor: Concert Pharmaceuticals
• Collaborators: Celerion

Study record dates

Study Major Dates

• Study Start (ACTUAL): September 5, 2019
• Primary Completion (ACTUAL): September 11, 2019
• Study Completion (ACTUAL): September 20, 2019

Study Registration Dates

• First Submitted: September 5, 2019
• First Submitted That Met QC Criteria: September 13, 2019
• First Posted (ACTUAL): September 17, 2019

Study Record Updates

• Last Update Posted (ACTUAL): September 25, 2019
• Last Update Submitted That Met QC Criteria: September 24, 2019
• Last Verified: September 1, 2019

More Information

Terms related to this study

• Keywords: Pharmacokinetics; Mass Balance; Radiolabeled
• Other Study ID Numbers: CP543.1004

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No