A Study to Assess Bioequivalence of Fezolinetant Formulations in Healthy Female Participants

NCT04277624 | Completed Phase 1 FDA Drug

• 1 other identifier: 2693-CL-0010
• Study Type: interventional
• Target: 22
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to assess the bioequivalence of a single dose of fezolinetant test formulation compared to a single dose of fezolinetant reference formulation under fasting conditions. This study will also evaluate the safety and tolerability of a single dose of fezolinetant test formulation and a single dose of fezolinetant reference formulation.

Conditions

Healthy Volunteers

Keywords

fezolinetant; ESN364; menopause

Outcome Measures

Primary Outcomes (3)

• Pharmacokinetics (PK) of fezolinetant in plasma: Area under the concentration-time curve (AUC) from the time of dosing extrapolated to time infinity (AUCinf)

  AUCinf will be recorded from the pharmacokinetic (PK) plasma samples collected

  Up to 72 hours postdose in each study period

• Pharmacokinetics (PK) of fezolinetant in plasma: Area under the concentration-time curve (AUC) from the time of dosing to the last measurable concentration (AUClast)

  AUClast will be recorded from the pharmacokinetic (PK) plasma samples collected

  Up to 72 hours postdose in each study period

• Pharmacokinetics (PK) of fezolinetant in plasma: Maximum concentration (Cmax)

  Cmax will be recorded from the pharmacokinetic (PK) plasma samples collected

  Up to 72 hours postdose in each study period

Secondary Outcomes (3)

• Number of participants with Adverse Events (AEs)

  Up to 19 days

• Number of participants with laboratory value abnormalities and/or adverse events (AEs)

  Up to 19 days

• Number of participants with vital sign abnormalities and/or adverse events (AEs)

  Up to 19 days

Study Arms (2)

Fezolinetant: Test Formulation then Reference Formulation

EXPERIMENTAL

Participants will receive a single oral dose of fezolinetant test formulation on day 1 of study period 1. After a washout of 5 days the participants will receive a single oral dose of fezolinetant reference formulation on day 1 of study period 2.

Drug: fezolinetant - test formulation; Drug: fezolinetant - reference formulation

Fezolinetant: Reference Formulation then Test Formulation

EXPERIMENTAL

Participants will receive a single oral dose of fezolinetant reference formulation on day 1 of study period 1. After a washout of 5 days the participants will receive a single oral dose of fezolinetant test formulation on day 1 of study period 2.

Drug: fezolinetant - test formulation; Drug: fezolinetant - reference formulation

Interventions

fezolinetant - test formulation DRUG

Administered orally

Also known as: ESN364

Fezolinetant: Reference Formulation then Test Formulation; Fezolinetant: Test Formulation then Reference Formulation

fezolinetant - reference formulation DRUG

Administered orally

Also known as: ESN364

Fezolinetant: Reference Formulation then Test Formulation; Fezolinetant: Test Formulation then Reference Formulation

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: female
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Subject is a healthy female subject.
• Subject has a body mass index (BMI) range of 18.5 to 34.0 kg/m\^2, inclusive and weighs at least 50 kg at screening.
• Postmenopausal female subjects only: Subject is postmenopausal according to 1 of the following criteria:
• Spontaneous amenorrhea for ≥ 12 consecutive months
• Spontaneous amenorrhea for ≥ 6 months with biochemical criteria of menopause (follicle-stimulating hormone \[FSH\] \> 40 IU/L); or
• Having had bilateral oophorectomy ≥ 6 weeks prior to the screening visit (with or without hysterectomy)
• Subject agrees not to participate in another interventional study while participating in the present study.
• Premenopausal female subjects only: Subject has had a regular menstrual cycle (from 25 to 31 days ± 3 days) for 3 months prior to starting the IP administration.
• Premenopausal female subjects only: Subject is not pregnant and at least meets 1 of the following criteria:
• If the subject is not of childbearing potential: Subject has lost fertility permanently by surgery excluding oophorectomy (e.g., hysterectomy, bilateral salpingectomy).
• If the subject is a woman of childbearing potential (WOCBP): Subject agrees to follow the contraceptive guidance from the time of providing informed consent through at least 30 days after the final IP administration. However, if the subject's partner has lost fertility by surgery (vasectomy or bilateral orchiectomy) etc., confirmed with documentation of both the procedure and absence of sperm, it is not necessary to implement contraceptive methods.
• Note: If absence of sperm cannot be confirmed in the subject's partner who received a vasectomy, an alternative contraceptive method must be used.
• Premenopausal female subjects only: Subject agrees not to breastfeed or donate ova from the time of providing informed consent until 30 days after the last IP administration.

You may not qualify if:

• Subject has received any investigational therapy within 28 days or 5 half-lives, whichever is longer, prior to screening.
• Subject has any condition which makes the subject unsuitable for study participation.
• Subject has a known or suspected hypersensitivity to fezolinetant or any components of the formulations used.
• Subject has had previous exposure with fezolinetant.
• Subject has any of the liver function tests (alkaline phosphatase \[ALP\], alanine aminotransferase \[ALT\], aspartate aminotransferase \[AST\] and total bilirubin \[TBL\]) \> 1.5 × upper limit of normal (ULN) on day -1. In such a case, the assessment may be repeated once.
• Subject has any clinically significant history of allergic conditions (including drug allergies, asthma, eczema or anaphylactic reactions, but excluding untreated, asymptomatic, seasonal allergies) prior to first investigational product (IP) administration.
• Subject has any history or evidence of any clinically significant cardiovascular, gastrointestinal, endocrinologic, hematologic, hepatic, immunologic, metabolic, urologic, pulmonary, neurologic, dermatologic, psychiatric, renal and/or other major disease or malignancy.
• Subject has/had febrile illness or symptomatic, viral, bacterial (including upper respiratory infection) or fungal (noncutaneous) infection within 1 week prior to day -1.
• Subject has any clinically significant abnormality following the physical examination, electrocardiogram (ECG) and protocol-defined clinical laboratory tests at screening or on day -1.
• Subject has a mean pulse \< 45 or \> 90 bpm or hypertension as defined by a systolic blood pressure ≥ 130 mmHg or diastolic blood pressure ≥ 80 mmHg based on the average of 3 readings on at least 2 different occasions during the screening period.
• Subject has a mean corrected QT interval using Fridericia's formula (QTcF) of \> 470 msec on day -1. If the mean QTcF exceeds the limits above, 1 additional triplicate ECG may be taken.
• Subject has used any prescribed or nonprescribed drugs (including vitamins, contraception \[oral, injectable, implantable or transdermal\] and natural and herbal remedies, e.g., St. John's Wort) in the 2 weeks prior to first IP administration and for hormone replacement therapy (HRT) in the 8 weeks prior to first IP administration, except for occasional use of acetaminophen (up to 2 g/day) and topical dermatological products, including corticosteroid products.
• Subject has smoked, used tobacco-containing products and nicotine or nicotine-containing products (e.g., electronic vapes) within 6 months prior to screening.
• Subject has a history of consuming \> 7 units of alcoholic beverages per week within 6 months prior to screening or has a history of alcoholism or drug/chemical/substance abuse within 2 years prior to screening (note: 1 unit = 12 ounces of beer, 4 ounces of wine, 1 ounce of spirits/hard liquor) or the subject tests positive for alcohol at screening or on day -1.
• Subject has used any drugs of abuse (amphetamines, barbiturates, benzodiazepines, cannabinoids, cocaine and/or opiates) within 3 months prior to day -1 or the subject tests positive for drugs of abuse (amphetamines, barbiturates, benzodiazepines, cannabinoids, cocaine and opiates) at screening or on day -1.

Sponsors & Collaborators

• Astellas Pharma Global Development, Inc.: lead

Study Sites (1)

PAREXEL Early Phase Clinical Unit

Baltimore, Maryland, 21225, United States

Location

MeSH Terms

Interventions

fezolinetant

Study Officials

• Executive Medical Director

  Astellas Pharma Global Development, Inc.

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 18, 2020
• First Posted: February 20, 2020
• Study Start: February 20, 2020
• Primary Completion: February 21, 2021
• Study Completion: February 26, 2021
• Last Updated: October 18, 2024

Record last verified: 2024-10

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)