A study to learn how safe elinzanetant is, how it affects the body, and how it moves into, through and out of the body after single and multiple doses in Japanese healthy female adults

JRCT ID: jRCT2071210049

Registered date:30/07/2021

Basic Information

• Recruitment status: Complete
• Health condition(s) or Problem(s) studied: Vasomotor Symptoms as a sex-hormone dependent disorder in women and men
• Date of first enrollment: 11/08/2021
• Target sample size: 62
• Study type: Interventional

Intervention(s)

Experimental: Elinzanetant single dose step 1
Each participant will receive a single oral dose of elinzanetant or placebo.
Experimental: Elinzanetant single dose step 2
Each participant will receive a single oral dose of elinzanetant or placebo.
Experimental: Elinzanetant single dose step 3
Each participant will receive a single oral dose of elinzanetant or placebo.
Experimental: Elinzanetant single dose step 4
Each participant will receive a single oral dose of elinzanetant or placebo.
Experimental: Elinzanetant single dose step 5
Each participant will receive multiple doses of elinzanetant or placebo administered once a day
for 7 consecutive days.
Experimental: Elinzanetant single dose step 6
Each participant will receive a single oral dose of elinzanetant or placebo.

Outcome(s)

• Primary Outcome: Number of participants with and severity of treatment-emergent adverse events (TEAEs) [Time Frame: Up to 2 weeks after start of dosing]

Secondary Outcome

Dose step 1 to 4, 6:
Cmax (maximum observed drug concentration after single dose administration) of elinzanetant [Time Frame: Day 1 pre-dose until 144 hours post-dose]
Cmax/D (Cmax divided by dose) of elinzanetant [Time Frame: Day 1 pre-dose until 144 hours post-dose]
AUC (area under the concentration vs. time curve from zero to infinity after single dose) of elinzanetant [Time Frame: Day 1 pre-dose until 144 hours post-dose]
AUC/D (AUC divided by dose) of elinzanetant [Time Frame: Day 1 pre-dose until 144 hours post-dose]

Dose step 5:
Cmax,md (maximum observed drug concentration after multiple dose administration) of elinzanetant [Time Frame: Day 7 (pre-dose until 144 hours post-dose)]
Cmax,md/D (Cmax,md divided by dose) of elinzanetant [Time Frame: Day 7 (pre-dose until 144 hours post-dose)]
AUC(0-24)md (AUC from time 0 to 24 h after multiple dose) of elinzanetant [Time Frame: Day 7 (pre-dose until 24 hours post-dose)]
AUC(0-24)md/D (AUC(0-24)md divided by dose) of elinzanetant [Time Frame: Day 7 (pre-dose until 24 hours post-dose)]

Key inclusion & exclusion criteria

• Age minimum: >= 40age old
• Age maximum: <= 65age old
• Gender: Female

Include criteria

- Japanese participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, blood pressure, pulse rate, 12 lead electrocardiogram (ECG), body temperature, and laboratory tests.
- Non-smoker, at least from 3 months before the screening visit onwards.
- Body weight of at least 40 kg and body mass index (BMI)
within the range 18.0 and 30.0 kg/m^2 (inclusive).

Exclude criteria

- Pregnant or breastfeeding women.
- Any clinically relevant abnormal findings in medical history and physical examination.
- History or evidence of any clinically relevant cardiovascular, gastrointestinal, endocrine, hematologic, hepatic, immunologic, metabolic, urologic, pulmonary, neurologic, dermatologic, psychiatric, renal and/or other clinically relevant disease.
- Relevant diseases or febrile illness within the last 4 weeks prior to the first study intervention administration.
- Regular use of medicines, or dietary supplements or other substances, e.g., carnitine products, anabolics, high dose vitamins.
- Use of any systemic or topical medicine or substance within 4 weeks before first study drug intervention, which oppose the study objectives, or which might influence them. This includes medicines and natural remedies (e.g St. Johns wort) that are altering the activity of CYP3A4 enzyme and the transporters Breast Cancer Resistance Protein (BCRP) and P-gp.
- ECG PR interval 210 msec, QT interval corrected using Bazetts formula (QTCB) 450 msec, QRS duration 110 msec at screening visit.
- ECG: PR interval > 210 msec, QT interval corrected using Bazetts formula (QTcB) >450 msec, QRS duration > 110 msec at screening visit.
- Systolic blood pressure below 90 or above 140 mmHg;
diastolic blood pressure below 40 or above 90 mmHg at
screening visit.
- Pulse rate below 50 or above 90 beats per minute (bpm; a lower pulse rate between 45 and 50 bpm is acceptable in case of normal thyroid function and absence of symptoms of bradycardia) at screening visit.
- Participants with a presence of any of the following, confirmed by a repeat test: aspartate aminotransferase (AST), alanine aminotransferase (ALT) and/or bilirubin above 1.2 x upper limit of normal (ULN) at screening visit.
- Participants with a presence of gamma-glutamyl transferase (GGT) > ULN confirmed by a repeat test, CK (creatine kinase) >2x ULN, and thyroid-stimulating hormone (TSH) outside normal range at screening visit.
- History of COVID-19 (coronavirus disease 2019).
- Suspected or confirmed active or prior SARS-CoV-2 (severe acute respiratory syndrome coronavirus type 2) infection according to local guidelines/practice.
- Contact with SARS-CoV-2- positive or COVID-19 patient within the last 4 weeks prior to admission to the study site.
- Positive SARS-CoV-2 viral RNA (ribonucleic acid) test.
- Vaccination against SARS-CoV-2 within 14 days before first administration of the study intervention or vaccination planned before completion of the last study visit.

Related Information

• Primary Sponsor: Myoishi Masashi
• Secondary ID(s): NCT04981431