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Completed

NCT Number: NCT03100591

A Study to Evaluate ACT-132577 in Healthy Male Subjects

The primary purpose of this study is to investigate the rate and routes (urine and feces) of elimination of ACT-132577, and the mass balance in urine and feces

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Key information

Conditions

Age range

45 year–65 year

Sex eligibility

Male

Study type

Interventional

Phase

Phase 1

Primary location

PRA Health Sciences

Groningen, Netherlands

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Signed informed consent in a language understandable to the subject prior to any study-mandated procedure;
  • Healthy male subjects aged between 45 and 65 years (inclusive) at screening;
  • Body mass index of 18.0 to 28.0 kg/m2 (inclusive) at screening;
  • Healthy on the basis of physical examination, cardiovascular assessments and laboratory tests.

Exclusion criteria

  • Values of hepatic aminotransferase (alanine aminotransferase and/or aspartate aminotransferase) > 3 × upper limit of normal range at screening;
  • Hemoglobin < 100 g/L at screening;
  • Known hypersensitivity to ACT-132577 or drugs of the same class, or any excipient of the ACT-132577 drug formulation;
  • Known hypersensitivity or allergy to natural rubber latex;
  • Previous exposure to ACT-132577;
  • Treatment with another investigational drug within 3 months prior to screening or participation in more than 4 investigational drug studies within 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;
  • A radiation burden of > 0.1 milliSievert (mSv) and ≤ 1.0 mSv in the period of 1 year prior to screening; a radiation burden of ≥ 1.1 mSv and ≤ 2.0 mSv in the period of 2 years prior to screening, etc. (add 1 year per 1 mSv).

Treatment and study plan

14C-radiolabeled ACT-132577

Drug

Single oral dose of 3.7 megabecquerel (MBq) (100 microcurie [μCi]) 14C-radiolabeled ACT-132577 administered as 1 capsule of 25 mg

Other names: Aprocitentan

Primary outcomes

  1. Cumulative excretion of radioactivity in urine and feces

    Time frame: From study treatment administration up to day 15

    14C-radioactivity will be measured daily in urine and feces samples for determination of total radioactivity recovery

Secondary outcomes

  1. Number of subjects with treatment-emergent adverse events and serious adverse events

    Time frame: From study treatment administration up to day 32

    Collection of any adverse event at each dose level

  2. Maximum plasma concentration (Cmax) of 14C-radiolabeled ACT-132577

    Time frame: From study treatment administration up to day 15

    Cmax is directly derived from the observed plasma concentrations of ACT-132577 and its metabolites

  3. Time to reach Cmax (tmax) of 14C-radiolabeled ACT-132577

    Time frame: From study treatment administration up to day 15

    tmax is directly derived from the observed plasma concentrations of ACT-132577 and its metabolites

  4. Terminal half-life (t1/2) of 14C-radiolabeled ACT-132577

    Time frame: From study treatment administration up to day 15

    t1/2 is calculated from the terminal rate constant obtained from the plasma concentrations-time curves of ACT-132577 and its metabolites

  5. Area under the plasma concentration-time curve (AUC) of 14C-radiolabeled ACT-132577

    Time frame: From study treatment administration up to day 15

    AUC is defined for the time intervals from zero to time t of the last measured concentration above the limit of quantification and from zero to infinity

  6. Maximum plasma concentration (Cmax) of ACT-132577 and its metabolites

    Time frame: From study treatment administration up to day 15

    Cmax is directly derived from the observed plasma concentrations of ACT-132577 and its metabolites

  7. Time to reach Cmax (tmax) of ACT-132577 and its metabolites

    Time frame: From study treatment administration up to day 15

    tmax is directly derived from the observed plasma concentrations of ACT-132577 and its metabolites

  8. Terminal half-life (t1/2) of ACT-132577 and its metabolites

    Time frame: From study treatment administration up to day 15

    t1/2 is calculated from the terminal rate constant obtained from the plasma concentrations-time curves of ACT-132577 and its metabolites

  9. Area under the plasma concentration-time curve (AUC) ACT-132577 and its metabolites

    Time frame: From study treatment administration up to day 15

    AUC is defined for the time intervals from zero to time t of the last measured concentration above the limit of quantification and from zero to infinity

Sponsors and collaborators

Lead sponsor

Idorsia Pharmaceuticals Ltd.

Industry

Registry information

Official study title

Single-center, Open-label Study With 14C-radiolabeled ACT-132577 to Investigate the Mass Balance, Pharmacokinetics, and Metabolism Following Single Oral Administration to Healthy Male Subjects

Important dates

Study start
2017
Primary completion
2017
Study completion
2017
First posted
Apr 4, 2017
Registry last updated
Nov 29, 2022

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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