Pharmacokinetics of Amcenestrant in Female Hepatic Impaired Participants as Compared to Participants With Normal Hepatic Function

NCT05126329 | Terminated Phase 1

• 3 other identifiers: POP16301U1111-1244-19292021-001784-24
• Study Type: interventional
• Target: 13
• Locations: 2 countries
• Sites: 3

Brief Summary

This is a Phase 1, parallel, open-label, 3-arm study to investigate the pharmacokinetic (PK) parameters of amcenestrant in female participants aged 40 to 75 years with mild and moderate hepatic impairment, and in matched participants with normal hepatic function.

Conditions

Hepatic Function Abnormal

Outcome Measures

Primary Outcomes (2)

• Pharmacokinetic (PK) assessment: Maximum plasma concentration observed (Cmax)

  Maximum plasma concentration observed (Cmax) of amcenestrant

  From Day 1 to Day 5

• PK assessment: Area under the plasma concentration (AUC)

  Area under the plasma concentration versus time curve of amcenestrant

  From Day 1 to Day 5

Secondary Outcomes (8)

• PK assessment: Tmax of amcenestrant

  From Day 1 to Day 5

• PK assessment: Area under the plasma concentration versus time curve (AUClast) of amcenestrant

  From Day 1 to Day 5

• PK assessment: Maximum unbound plasma concentration (Cmax u) of amcenestrant

  From Day 1 to Day 5

• PK assessment: AUCu of amcenestrant

  From Day 1 to Day 5

• PK assessment: Cmax of M7

  From Day 1 to Day 5

Study Arms (3)

Participants with mild hepatic impairment

EXPERIMENTAL

Amcenestrant 200 mg single dose on Day 1 in fed condition

Drug: amcenestrant

Participants with moderate hepatic impairment

EXPERIMENTAL

Amcenestrant 200 mg single dose on Day 1 in fed condition

Drug: amcenestrant

Participants with normal hepatic function

EXPERIMENTAL

Amcenestrant 200 mg single dose on Day 1 in fed condition

Drug: amcenestrant

Interventions

amcenestrant DRUG

tablet for oral use

Participants with mild hepatic impairment; Participants with moderate hepatic impairment; Participants with normal hepatic function

Eligibility Criteria

• Age: 40 Years - 75 Years
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• For participants with hepatic impairment:
• Participant must be 40 to 75 years of age, inclusive.
• Female participants who are postmenopausal or are post-bilateral surgical oophorectomy not linked to a history of cancer. Menopause is defined as being amenorrheic for at least 12 months without an alternative medical cause, with plasma FSH level \>30 IU/L or age ≥60 years.
• Stable chronic liver disease assessed by medical history, physical examination, laboratory values
• Body weight within the range 50 kg (40 kg for site in South Korea) to 110 kg and body mass index (BMI) within the range 18 to 36 kg/m2, inclusive.
• For moderate hepatic impairment cohort: Child-Pugh total score ranging from 7 to 9, inclusive.
• For mild hepatic impairment cohort: Child-Pugh total score ranging from 5 to 6, inclusive
• For matched subjects:
• Participant must be 40 to 75 years of age, inclusive.
• Female participants who are postmenopausal or are post-bilateral surgical oophorectomy not linked to a history of cancer. Menopause is defined as being amenorrheic for at least 12 months without an alternative medical cause, with plasma FSH level \>30 IU/L or age ≥60 years.
• Certified as healthy by a comprehensive clinical assessment (detailed medical history and complete physical examination).
• Body weight within the range 50 kg (40 kg for site in South Korea) to 100 kg and body mass index (BMI) within the range 18 to 36 kg/m2, inclusive.

You may not qualify if:

• For participants with hepatic impairment:
• Smoking regularly more than 15 cigarettes or equivalent per day, unable to refrain from smoking over 8 cigarettes per day during the institutionalization (Smoking is not allowed within 8 hours after amcenestrant administration).
• Excessive consumption of beverages containing xanthine bases (more than 5 cups or glasses per day).
• Use of any herbal medicines 1 week before IMP administration and up to the end of PK sampling following the IMP administration
• Treatment with a strong CYP3A, CYP2C8 or any UGTs inhibitor within 14 days before first study treatment administration or 5 half-lives whichever is longer.
• Treatment with a strong or moderate CYP3A, CYP2C8 or any UGTs inducer within 14 days before first study treatment administration or 5 half-lives whichever is longer.
• Uncontrolled clinically relevant cardiovascular, pulmonary, gastrointestinal, metabolic, hematological, neurological, psychiatric, systemic, ocular, gynecologic, renal, infectious disease, severe hepatic impairment (Child-Pugh total score greater than or equal to 10), or signs of acute illness, hepatocarcinoma, acute hepatitis, Hepatic encephalopathy Grade 2, 3, and 4
• For matched subjects:
• Smoking regularly more than 15 cigarettes or equivalent per day, unable to refrain from smoking over 8 cigarettes per day during the institutionalization (Smoking is not allowed within 8 hours after amcenestrant administration).
• Excessive consumption of beverages containing xanthine bases (more than 5 cups or glasses per day).
• Any history or presence of clinically relevant cardiovascular, pulmonary, gastrointestinal, hepatic, renal, metabolic, hematological, neurological, osteomuscular, articular, psychiatric, systemic, ocular, gynecologic, or infectious disease, or signs of acute illness, unless the Investigator considers an abnormality to be not clinically significant.
• Frequent headaches and/or migraine, recurrent nausea and/or vomiting (for vomiting only: more than twice a month.
• Treatment with a strong CYP3A, CYP2C8 or any UGTs inhibitor within 14 days before first study treatment administration or 5 half-lives whichever is longer.
• Treatment with a strong or moderate CYP3A, CYP2C8 or any UGTs inducer within 14 days before first study treatment administration or 5 half-lives whichever is longer.
• Use of any herbal medicines 1 week before IMP administration and up to the end of PK sampling following the IMP administration The above information is not intended to contain all considerations relevant to a patient's potential participation in a clinical trial

Sponsors & Collaborators

• Sanofi: lead

Study Sites (3)

Investigational Site Number :2760001

Kiel, 24105, Germany

Location

Investigational Site Number :4100001

Seoul, Seoul-teukbyeolsi, 03080, South Korea

Location

Investigational site number :4100002

Cheongju-si, 28644, South Korea

Location

Related Links

• POP16301 Plain Language Results Summary

MeSH Terms

Conditions

Liver Diseases

Condition Hierarchy (Ancestors)

Digestive System Diseases

Study Officials

• Clinical Sciences & Operations

  Sanofi

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: November 3, 2021
• First Posted: November 19, 2021
• Study Start: November 15, 2021
• Primary Completion: May 16, 2022
• Study Completion: May 16, 2022
• Last Updated: September 22, 2025

Record last verified: 2025-09

Data Sharing

• IPD Sharing: Will share

Locations

KR (2); DE (1)