A Study of the Absorption, Metabolism, and Excretion of [14C]-Brensocatib Following a Single Oral Administration in Healthy Male Participants

A Phase 1, Open-label Study of the Absorption, Metabolism, and Excretion of [14C]-Brensocatib Following a Single Oral Administration in Healthy Male Subjects

The primary purpose of the study is to determine the mass balance of total radioactivity and the routes of elimination by quantifying the urinary and fecal excretion of radioactivity following a single oral administration of [14C]-brensocatib, to characterize the pharmacokinetics (PK) of brensocatib in plasma and urine, PK of total radioactivity in plasma, whole blood, urine and to determine the blood-to-plasma ratios of total radioactivity.

Study Overview

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

• Study Type: Interventional
• Enrollment (Actual): 7
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Wisconsin
    • Madison, Wisconsin, United States, 53704
      • USA001

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

1. Body mass index between 18.0 and 32.0 kilograms per square meter (kg/m^2), inclusive, at screening.
2. In good health, determined by no clinically significant findings from medical history, physical examination, 12-lead electrocardiogram (ECG), vital sign measurements, and clinical laboratory evaluations (congenital nonhemolytic hyperbilirubinemia [eg, suspicion of Gilbert's syndrome based on total and direct bilirubin] is not acceptable) at screening and check-in as assessed by the investigator (or designee).

Exclusion Criteria:

1. Positive hepatitis panel and/or positive human immunodeficiency virus test. Results consistent with previous vaccination to Hepatitis B are not exclusionary.
2. Administration of a coronavirus disease 2019 (COVID-19) vaccine in the past 14 days prior to dosing.
3. Poor peripheral venous access.
4. Have previously completed or withdrawn from this study or any other study investigating brensocatib, and have previously received brensocatib. Known allergy to brensocatib or any of the excipients used in the formulation.
5. Exposure to significant diagnostic or therapeutic radiation (e.g., serial X-ray, computed tomography scan, barium meal) or current employment in a job requiring radiation exposure monitoring within 12 months prior to check-in.
6. Participated in more than 3 radiolabeled drug studies in the last 12 months (previous study to be at least 4 months prior to check-in to the study site where exposures are known to the investigator or 6 months prior to check-in to the study site for a radiolabeled drug study where exposures are not known to the investigator).

Note: Other inclusion/exclusion criteria may apply.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: [14C]-brensocatib; Healthy participants will receive single oral dose of [14C]-brensocatib on Day 1 under fasted conditions.	Drug: [14C]-brensocatib; Oral solution.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Area Under the Concentration Time Curve (AUC) of Brensocatib in Plasma	Pharmacokinetics of brensocatib following a single dose in healthy participants will be assessed.	Pre-dose and at multiple timepoints post-dose on Day 1 up to maximum Day 14
AUC∞ Plasma Brensocatib/Plasma Total Radioactivity Ratio Calculated as AUC∞ of Plasma Brensocatib Relative to AUC∞ of Plasma Total Radioactivity		Pre-dose and at multiple timepoints post-dose on Day 1 up to maximum Day 14
AUC∞ Blood/Plasma Total Radioactivity Ratio Calculated as AUC∞ of Whole Blood Total Radioactivity to AUC∞ of Plasma Total Radioactivity		Pre-dose and at multiple timepoints post-dose on Day 1 up to maximum Day 14
Amount Excreted in Urine (Aeu) of Brensocatib		Pre-dose and at multiple timepoints post-dose on Day 1 up to maximum Day 14
Total Radioactivity Expressed as Amount of [14C]-brensocatib Excreted in Urine		Pre-dose and at multiple timepoints post-dose on Day 1 up to maximum Day 14
Total Radioactivity Expressed as Amount of [14C]-brensocatib Excreted in Feces (Aef)		Pre-dose and at multiple timepoints post-dose on Day 1 up to maximum Day 14

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
AUC of Brensocatib Metabolites in Plasma	Pharmacokinetics of the metabolites following a single dose of brensocatib in healthy participants will be assessed.	Pre-dose and at multiple timepoints post-dose on Days 1 to 9
Number of Participants Who Experienced at Least one Adverse Event (AE)	Safety and tolerability of a single dose of brensocatib will be determined in healthy participants.	Up to Day 14

Collaborators and Investigators

• Sponsor: Insmed Incorporated

Study record dates

Study Major Dates

• Study Start (Actual): August 13, 2021
• Primary Completion (Actual): September 14, 2021
• Study Completion (Actual): September 14, 2021

Study Registration Dates

• First Submitted: December 7, 2022
• First Submitted That Met QC Criteria: December 7, 2022
• First Posted (Actual): December 15, 2022

Study Record Updates

• Last Update Posted (Actual): March 23, 2023
• Last Update Submitted That Met QC Criteria: March 21, 2023
• Last Verified: March 1, 2023

More Information

Terms related to this study

• Keywords: [14C]-brensocatib
• Other Study ID Numbers: INS1007-103

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

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