A Study to Evaluate ACT-246475 Fate in Healthy Male Subjects

Single-center, Open-label Study With 14C-radiolabeled ACT-246475 to Investigate Its Mass Balance, Pharmacokinetics, and Metabolism Following Single Subcutaneous Administration to Healthy Male Subjects

The purpose of this study is to investigate how quickly and to what extent ACT-246475 is absorbed, distributed, metabolized (broken down) and eliminated from the body. ACT-246475 will be labeled with 14-Carbon (14C) and, in this way can be traced in blood, urine, and feces. This study will also investigate how safe is ACT-246475 and how well it is tolerated when administered to healthy male volunteers.

Study Overview

• Status: Completed
• Conditions: Healthy Subjects
• Intervention / Treatment: Drug: ACT-246475

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

Contacts and Locations

Study Locations

• Germany
  • Bad Krozingen, Germany, 79189
    • Universitäts-Herzzentrum Bad Krozingen
  • Freiburg, Germany, 79106
    • Universitats-Herzzentrum Freiburg
  • Ludwigshafen, Germany, 67063
    • Klinikum der Stadt Ludwigshafen am Rhein gGmbH

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 45 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Main Inclusion Criteria:

• Signed informed consent in the local language prior to any studymandated procedure,
• Healthy male subjects aged between 45 and 65 years (inclusive) at screening,
• No clinically significant findings on the physical examination at screening,
• Body mass index of 18.0-28.0 kg/m2 (inclusive) at screening,
• Systolic blood pressure (BP) 100-140 mmHg, diastolic BP 50-90 mmHg, and pulse rate 45-90 bpm (inclusive), measured on either arm, after 5 min in the supine position at screening,
• 12-lead electrocardiogram (ECG) without clinically relevant abnormalities, measured after 5 min in the supine position at screening,
• Values of closure time tested with the Platelet Function Analyzer equipment, for both cartridges of collagen/epinephrine and collagen/adenosine diphosphate below the upper limit of normal range at screening.

Main Exclusion Criteria:

• Known hypersensitivity to ACT-246475 or drugs of the same class, or any excipients of the ACT-246475 formulation,
• History or clinical evidence of any disease and/or existence of any surgical or medical condition, which might interfere with the absorption, distribution, metabolism or excretion of the study treatment (appendectomy and herniotomy allowed, cholecystectomy not allowed),
• Family or personal history of prolonged bleeding (e.g., after surgical intervention) or bleeding disorders (e.g., thrombocytopenia, clotting disturbances), intracranial vascular diseases, stroke, reasonable suspicion of vascular malformations, or peptic ulcers,
• Platelet count < 120 x10^9 L-1 at screening,
• Previous exposure to ACT-246475,
• Participation in another study with a radiation burden of > 0.1 mSv and ≤ 1.0 mSv in a period of 1 year prior to screening; a radiation burden of > 1 mSv and ≤ 2.0 mSv in a period of 2 years prior to screening, etc. (add 1 year per 1 mSv),
• Exposure to radiation for diagnostic reasons (except dental X-rays and plain X-rays of thorax and bony skeleton [excluding spinal column]), during work or during participation in a clinical study, in the period of 1 year prior to screening,
• Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• 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: Treatment and observation period; On Day 1, the subjects will receive a single s.c. dose of 16 mg 14C-radiolabeled ACT-246475 in the fasted state. Subjects will be followed by an observation period of 3 days (72 h) during which blood, urine, and feces samples will be collected.	Drug: ACT-246475; Single s.c. dose of 16 mg ACT-246475 including 3.7 MBq (100 μCi) 14C-radiolabeled ACT 246475

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cumulative excretion of total 14C-radioactivity in urine and feces	Cumulative amount of total 14C-radioactivity excreted in urine and feces will be calculated by summing up the amount of total 14C-radioactivity of the samples excreted in each collection interval	Up to 54 days

Collaborators and Investigators

• Sponsor: Idorsia Pharmaceuticals Ltd.

Study record dates

Study Major Dates

• Study Start (Actual): July 27, 2018
• Primary Completion (Actual): August 5, 2018
• Study Completion (Actual): August 5, 2018

Study Registration Dates

• First Submitted: July 10, 2018
• First Submitted That Met QC Criteria: July 10, 2018
• First Posted (Actual): July 20, 2018

Study Record Updates

• Last Update Posted (Actual): November 16, 2022
• Last Update Submitted That Met QC Criteria: November 15, 2022
• Last Verified: November 1, 2022

More Information

Terms related to this study

• Other Study ID Numbers: ID-076-104; 2017-004622-15 (EudraCT Number)

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