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Completed

NCT Number: NCT04940026

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

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

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Key information

Conditions

Breast Cancer Breast Diseases Breast Neoplasms Healthy Volunteers Neoplasms Neoplasms by Site Skin Diseases Skin and Connective Tissue Diseases

Age range

40 year–75 year

Sex eligibility

Female

Study type

Interventional

Phase

Phase 1

Primary location

Investigational Site Number 8260001

Nottingham, NG11 6JS, United Kingdom

About this study

Total study duration is 3 to 10 weeks, including a screening period of up to 27 days, treatment period of up to 16 days and a follow-up and end of study of up to 4 weeks.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

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.

Exclusion criteria

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).

Blood donation, any volume (usually approximately 500 mL), within 2 months before inclusion.

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.

Treatment and study plan

amcenestrant

Drug

Tablet Oral

Other names: SAR439859

[14C]-SAR439859 microtracer

Drug

Solution for infusion Intravenous

[14C]-SAR439859

Drug

Powder for oral solution Oral

Primary outcomes

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

    Time frame: Day 1 to Day 6

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

    Time frame: Day 7 up to max Day 44

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

    Time frame: Day 1 to Day 3

    Area under the plasma concentration versus time curve extrapolated to infinity

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

    Time frame: Day 1 to Day 3

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

  5. Assessment of PK parameter: CL for SAR439859 after IV administration

    Time frame: Day 1 to Day 3

    Total body clearance

  6. Assessment of PK parameter: AUC ratios after IV administration

    Time frame: Day 1 to Day 3

    SAR439859 to radioactivity ratio for plasma AUC

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

    Time frame: Day 1 to Day 5, Day 7 to Day 11

    Maximum plasm concentration observed

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

    Time frame: Day 1 to Day 5, Day 7 to Day 11

    Time to reach Cmax

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

    Time frame: Day 1 to Day 5, Day 7 to Day 11

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

    Time frame: Day 1 to Day 5, Day 7 to Day 11

  11. Assessment of PK parameter: AUC ratios after oral administration

    Time frame: Day 7 to Day 11

    SAR439859 to radioactivity ratio for plasma AUC

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

    Time frame: Day 1 to Day 5, Day 7 to Day 11

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

    Time frame: Day 1 to Day 5, Day 7 to Day 11

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

    Time frame: Day 1 to Day 5, Day 7 to Day 11

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

    Time frame: Day 1 to Day 5, Day 7 to Day 11

    M7 to SAR439859 ratio for plasma Cmax

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

    Time frame: Day 1 to Day 5, Day 7 to Day 11

    M7 to SAR439859 ratio for plasma AUC

  17. Absolute oral bioavailability of SAR439859

    Time frame: Day 1 to Day 5, Day 7 to Day 11

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

  18. Relative bioavailability of SAR439859 after oral administration

    Time frame: Day 1 to Day 5, Day 7 to Day 11

Secondary outcomes

  1. Number of participants with adverse events

    Time frame: Day 1 to Day 44

Sponsors and collaborators

Lead sponsor

Sanofi

Industry

Registry information

Official study title

A Phase 1, Open-label, Single Center, One Period, One Sequence Study to Determine Absorption, Metabolism, and Excretion of a Single Oral Dose of Radiolabeled [14C]- SAR439859 and an Assessment of the Absolute Oral Bioavailability Using the Microdosing Technique in Healthy Post-menopausal Women

Important dates

Study start
2021
Primary completion
2021
Study completion
2021
First posted
Jun 25, 2021
Registry last updated
Sep 24, 2025

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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