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

Sanofi1 个研究点分布在 1 个国家目标入组 6 人开始时间: 2021年6月15日最近更新: 2025年9月24日

适应症

干预措施

试验速览

阶段: 1 期
状态: 已完成
发起方: Sanofi
入组人数: 6
试验地点: 1
主要终点: Percentage of radioactive dose excreted in urine and feces after oral administration

研究概览研究设计入排标准研究组 & 干预措施结局指标研究者研究点记录与标识符相似试验

研究概览

简要总结

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

详细描述

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.

研究设计

研究类型: Interventional
分配方式: Na
干预模型: Single Group
主要目的: Other
盲法: None

入排标准

年龄范围: 40 Years 至 75 Years（Adult, Older Adult）
性别: Female
接受健康志愿者: 是

入选标准

•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.

排除标准

•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
•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.

研究组 & 干预措施

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

干预措施: amcenestrant (Drug)

SAR439859

Experimental

干预措施: [14C]-SAR439859 microtracer (Drug)

SAR439859

Experimental

干预措施: [14C]-SAR439859 (Drug)

结局指标

主要结局

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

时间窗: Day 7 up to max Day 44

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

时间窗: Day 1 to Day 3

Area under the plasma concentration versus time curve extrapolated to infinity

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

时间窗: Day 1 to Day 3

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

Assessment of PK parameter: AUC ratios after IV administration

时间窗: Day 1 to Day 3

SAR439859 to radioactivity ratio for plasma AUC

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