A Study to Investigate the Effect of ACT-132577 on the Pharmacokinetics of Midazolam and 1-hydroxy Midazolam in Healthy Male Subjects

A Single-center, Open-label, Two-treatment Study to Investigate the Effect of ACT-132577 at Steady State on the Pharmacokinetics of Midazolam and Its Metabolite 1-hydroxy Midazolam in Healthy Male Subjects

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT02841761

Enrollment

Registered

2016-07-22

Start date

2016-07-01

Completion date

2016-10-01

Last updated

2022-11-29

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Healthy Subjects

Brief summary

The purpose of this study is to evaluate the effect of ACT-132577 on the pharmacokinetics of midazolam and 1-hydroxy midazolam and to evaluate the safety and tolerability of ACT-132577 when administered alone and in combination with midazolam.

Interventions

DRUGMidalozam

Syrup for oral use

DRUGAprocitentan

Capsules for oral use

Study design

Allocation

NON_RANDOMIZED

Intervention model

PARALLEL

Primary purpose

OTHER

Masking

NONE

Eligibility

Sex/Gender

MALE

Age

18 Years to 45 Years

Healthy volunteers

Yes

Inclusion criteria

* Signed informed consent in the local language prior to any study-mandated procedure * Body mass index (BMI) of 18.0 to 30.0 kg/m2 (inclusive) at screening * Healthy on the basis of medical history, physical examination, cardiovascular assessments and serology and laboratory tests

Exclusion criteria

* Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol

Design outcomes

Primary

Measure	Time frame	Description
Maximum observed plama concentration (Cmax)	Midazolam PK sampling on Days 1, 2, 6 and 7	Cmax of midazolam and 1-hydroxy midazolam following administration of midazolam alone and in combination with ACT-132577
Area under the plasma concentration-time curve from zero to infinity (AUC0-∞)	Midazolam PK sampling on Days 1, 2, 6 and 7	AUC0-∞ of midazolam and 1-hydroxy midazolam following administration of midazolam alone and in combination with ACT-132577
Time to reach Cmax (tmax)	Midazolam PK sampling on Days 1, 2, 6 and 7	Tmax of midazolam and 1-hydroxy midazolam following administration of midazolam alone and in combination with ACT-132577
Terminal half-life (t1/2)	Midazolam PK sampling on Days 1, 2, 6 and 7	T1/2 of midazolam and 1-hydroxy midazolam following administration of midazolam alone and in combination with ACT-132577

Secondary

Measure	Time frame
Number of subjects with adverse events	From Day 1 to Follow-up (for up to 38 days)
Number of subjects with serious adverse events	From Screening to Follow-up (for up to 59 days)

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026