Study to Determine Absorption, Metabolism, and Excretion of [14C]-SAR439859, and to Assess Absolute Oral Bioavailability of Amcenestrant (SAR439859), in Healthy Post-menopausal Women

NCT04940026 | Completed Phase 1

• 1 other identifier: BEX15859
• Study Type: interventional
• Target: 6
• Locations: 1 country
• Sites: 1

Brief Summary

Primary Objectives:

• To assess the excretion balance after oral and IV administration of \[14C\]-SAR439859
• To assess PK of total radioactivity, \[14C\] -SAR439859 and its metabolite (M7) after IV administration of \[14C\]-SAR439859 and, PK of radioactivity, SAR439859 and M7 after oral administration of SAR439859 alone or with \[14C\]-SAR439859
• To assess IV clearance and absolute bioavailability of SAR439859 using microdose of \[14C\]-SAR439859 tracer on top of a single tablet oral dose.
• To assess relative bioavailability of SAR439859 given as tablet or solution Secondary objectives:
• To collect samples in order to assess metabolic profile in plasma and excreta of SAR439859 after oral administration of \[14C\]-SAR439859 as solution, contribution in plasma of SAR439859 and metabolite relative to total radioactivity and identify metabolites (samples will be analyzed according to metabolic analysis plan and results will be documented in a separate report).
• To assess safety and tolerance of SAR439859

Conditions

Breast Cancer; Healthy Volunteers

Outcome Measures

Primary Outcomes (18)

• Percentage of radioactive dose, SAR439859 and M7 excreted in urine and feces after IV administration

  Day 1 to Day 6

• Percentage of radioactive dose excreted in urine and feces after oral administration

  Day 7 up to max Day 44

• Assessment of Pharmacokinetic (PK) parameter: AUC for radioactivity and SAR439859 after IV administration

  Area under the plasma concentration versus time curve extrapolated to infinity

  Day 1 to Day 3

• Assessment of PK parameter: t1/2z for radioactivity and SAR439859 after IV administration

  Terminal half-life associated with the terminal slope (λz)

  Day 1 to Day 3

• Assessment of PK parameter: CL for SAR439859 after IV administration

  Total body clearance

  Day 1 to Day 3

• Assessment of PK parameter: AUC ratios after IV administration

  SAR439859 to radioactivity ratio for plasma AUC

  Day 1 to Day 3

• Assessment of PK parameter: Cmax for radioactivity and SAR439859 after oral administration

  Maximum plasm concentration observed

  Day 1 to Day 5, Day 7 to Day 11

• Assessment of PK parameter: tmax for radioactivity and SAR439859 after oral administration

  Time to reach Cmax

  Day 1 to Day 5, Day 7 to Day 11

• Assessment of PK parameter: AUC for radioactivity and SAR439859 after oral administration

  Day 1 to Day 5, Day 7 to Day 11

• Assessment of PK parameter: t1/2z for radioactivity and SAR439859 after oral administration

  Day 1 to Day 5, Day 7 to Day 11

• Assessment of PK parameter: AUC ratios after oral administration

  SAR439859 to radioactivity ratio for plasma AUC

  Day 7 to Day 11

• Assessment of PK parameter: Cmax for M7 after IV and oral administration

  Day 1 to Day 5, Day 7 to Day 11

• Assessment of PK parameter: AUC for M7 after IV and oral administration

  Day 1 to Day 5, Day 7 to Day 11

• Assessment of PK parameter: t1/2z for M7 after IV and oral administration

  Day 1 to Day 5, Day 7 to Day 11

• Assessment of PK parameter: Rmet Cmax after IV and oral administration

  M7 to SAR439859 ratio for plasma Cmax

  Day 1 to Day 5, Day 7 to Day 11

• Assessment of PK parameter: Rmet AUC after IV and oral administration

  M7 to SAR439859 ratio for plasma AUC

  Day 1 to Day 5, Day 7 to Day 11

• Absolute oral bioavailability of SAR439859

  Absolute oral bioavailability, expressed as a percentage, estimated from AUCs obtained after oral and IV administration

  Day 1 to Day 5, Day 7 to Day 11

• Relative bioavailability of SAR439859 after oral administration

  Day 1 to Day 5, Day 7 to Day 11

Secondary Outcomes (1)

• Number of participants with adverse events

  Day 1 to Day 44

Study Arms (1)

SAR439859

EXPERIMENTAL

Single oral dose of SAR439859 at Day 1 in fasted condition followed by intravenous administration of \[14C\]-SAR439859 microtracer 3 hours later, and single oral dose of \[14C\]-SAR439859 at Day 7 in fasted condition

Drug: amcenestrant; Drug: [14C]-SAR439859 microtracer; Drug: [14C]-SAR439859

Interventions

amcenestrant DRUG

Tablet Oral

Also known as: SAR439859

SAR439859

[14C]-SAR439859 microtracer DRUG

Solution for infusion Intravenous

SAR439859

[14C]-SAR439859 DRUG

Powder for oral solution Oral

SAR439859

Eligibility Criteria

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

You may qualify if:

• Female participants (age between 40 and 75 years old) who are postmenopausal or had post-bilateral surgical oophorectomy not linked to a history of cancer.
• Participants who are overtly healthy. Body weight within 40.0 and 95.0 kg and body mass index (BMI) within the range 18.0 and 30 kg/m2 (inclusive).
• Capable of giving signed informed consent.

You may not qualify if:

• Subject has clinical signs and symptoms consistent with COVID-19, e.g., fever, dry cough, dyspnea, loss of taste and smell, sore throat, fatigue or confirmed infection by appropriate laboratory test within the last 4 weeks prior to Screening.
• Subject who had severe course of COVID-19 (i.e., hospitalization, extracorporeal membrane oxygenation, mechanically ventilated).
• Frequent headaches and/or migraine, recurrent nausea and/or vomiting (for vomiting only: more than twice a month).
• Presence or history of drug hypersensitivity, or allergic disease diagnosed and treated by a physician.
• History or presence of drug or alcohol abuse (alcohol consumption more than 40 g per day).
• Smoking regularly more than 5 cigarettes or equivalent per week, unable to stop smoking during the study (occasional smoker can be enrolled).
• Excessive consumption of beverages containing xanthine bases (more than 5 cups or glasses per day).
• Subjects who are occupationally exposed to radiation as defined in the Ionizing Radiation Regulations 2017.
• Participation in a trial with \[13C\] or \[14C\] radiolabeled medication in the 12 months preceding the study.
• 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 (1)

Investigational Site Number 8260001

Nottingham, NG11 6JS, United Kingdom

Location

Related Links

• BEX15859 Plain Language Results Summary

MeSH Terms

Conditions

Breast Neoplasms

Condition Hierarchy (Ancestors)

Neoplasms by Site; Neoplasms; Breast Diseases; Skin Diseases; Skin and Connective Tissue Diseases

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: OTHER
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: June 14, 2021
• First Posted: June 25, 2021
• Study Start: June 15, 2021
• Primary Completion: August 19, 2021
• Study Completion: August 19, 2021
• Last Updated: September 24, 2025

Record last verified: 2025-09

Data Sharing

• IPD Sharing: Will share

Locations

GB (1)