Sleeping disorders insomnia Sleeping disorders
Conditions
Interventions
Oral dose administration of ACT-541468 (25 and 50 mg) on Day 1 till Day 5. An
optional 3rd cohort (10 mg) will be initiated when differences in results are
observed between the Japanese and the Cauc
Orexin antagonist
PK & PD
Safety & tolerability
Sleeping disorder
Sponsors
Actelion Pharmaceuticals
Eligibility
Age
18 Years to 64 Years
Inclusion criteria
Inclusion criteria: - Signed informed consent prior to any study-mandated procedure. - Healthy male and female subjects aged between 20 and 50 years (inclusive) at screening. - A woman of childbearing potential must provide: - Negative serum pregnancy test at screening. - Negative urine pregnancy test at Day 1. - Agreement to undertake pregnancy tests up to 30 days after EOT. - No clinically significant findings on the physical examination at screening. - Body mass index of 18.0 to 26.0 kg/m2 (inclusive) at screening. - Systolic blood pressure (SBP) 100-145 mmHg, diastolic blood pressure (DBP) 50-90 mmHg, and pulse rate 45-90 bpm (inclusive), measured on either arm, after 5 min in the supine position at screening and at Day 1 pre dose. - 12-lead electrocardiogram (ECG) without clinically relevant abnormalities, measured after 5 min in the supine position at screening and at Day 1 pre-dose. - Hematology, clinical chemistry, and urinalysis test results not deviating from the normal range to a clinically relevant extent at screening. - Negative results from urine drug screen and alcohol breath test at screening and Day 1. - Ability to communicate well with the investigator, in the local language (Dutch, English, or Japanese), and to understand and comply with the requirements of the study. - Subjects must be of Caucasian or Japanese ethnicity.;Japanese subjects only: - Subjects must be of native Japanese descent (all parents/grandparents of Japanese descent). * Subjects must not have been away from Japan for more than 10 years (at screening visit). * Subject's lifestyle should not have changed significantly since relocation from Japan.
Exclusion criteria
Exclusion criteria: - Known hypersensitivity to ACT-541468 or drugs of the same class, or any of the excipients. - Previous exposure to the study drug. - Known hypersensitivity or allergy to natural rubber latex. - 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). - Previous relevant history of fainting, collapse, syncope, orthostatic hypotension, or vasovagal reactions. - Modified Swiss Narcolepsy Scale total score 800 mg per day at screening. - Nicotine intake (e.g., smoking, nicotine patch, nicotine chewing gum, or electronic cigarettes) within 3 months prior to screening and inability to refrain from nicotine intake from screening until End-of-Study (EOS). - Treatment with another investigational treatment within 3 months prior to screening or participation in more than 4 investigational treatment studies within 1 year prior to screening. - Previous treatment with any prescribed medications (including all type of vaccines) or over-the-counter (OTC) medications (including herbal medicines such as St John*s Wort, homeopathic preparations, vitamins, and minerals) within 2 weeks or 5 half-lives (whichever is longer) prior to first study treatment administration. - Loss of 250 mL or more of blood within 3 months prior to screening. - Positive results from the hepatitis serology, except for vaccinated subjects or subjects with past but resolved hepatitis, at screening. - Positive results from the HIV serology at screening. - Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol. - Legal incapacity or limited legal capacity at screening.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Safety and tolerability: clincal relevant changes in lab, ECG, vital parameters. (S)AE's. PK: Cmax, Tmax, T1/2, AUC0-8, AUC0-24, Accumulation index PD: change from baseline of pharmacodynamic assessments. | — |
Countries
The Netherlands
Outcome results
None listed