此页面是自动翻译的,不保证翻译的准确性。请参阅 英文版 对于源文本。

Pharmacokinetics and Excretion of [¹⁴C]Etelcalcetide (AMG 416) in Patients With End Stage Renal Disease (ESRD) Receiving Dialysis

2018年8月2日 更新者:Amgen

An Open-label, Single-dose Study to Evaluate the Pharmacokinetics, Biotransformation and Excretion of [¹⁴C]AMG 416 in Patients With End Stage Renal Disease Receiving Dialysis

The primary objectives of this study were to determine the rate, extent, and routes of radioactivity excretion of [¹⁴C]etelcalcetide in feces, dialysate, and urine over time and to measure radioactivity concentrations in whole blood and plasma over time.

研究概览

详细说明

Six adult male or female patients with end stage renal disease requiring hemodialysis will be enrolled to receive 750 nCi of [¹⁴C]-labeled etelcalcetide formulated in 10 mg etelcalcetide administered as a single 2 mL intravenous dose at the end of hemodialysis.

Participants will spend the first approximately 12 days in confinement at the clinic (day -1 until completion of day 11 study procedures). Blood samples, and complete collections of dialysate, dialysis membrane (as necessary), urine (as available), and feces will be analyzed for radioactivity content by accelerator mass spectrometry (AMS). Following the confinement period, participants will return to the site on an outpatient basis in accordance to their routine dialysis sessions up to day 39. Blood and dialysate samples and dialysis membranes will be collected at specified times during the outpatient visit period.

Participants may be asked to return so the site for the Extended Pharmacokinetic Collection Period. During the Extended Pharmacokinetic Collection Period, participants will return to the site for 3 consecutive hemodialysis sessions (Collection Period 1) and then again approximately one month later, for an additional 3 consecutive hemodialysis sessions (Collection Period 2).

研究类型

介入性

注册 (实际的)

6

阶段

  • 阶段1

联系人和位置

本节提供了进行研究的人员的详细联系信息,以及有关进行该研究的地点的信息。

学习地点

    • Minnesota
      • Minneapolis、Minnesota、美国、55404
        • Davita Clinical Research Center

参与标准

研究人员寻找符合特定描述的人,称为资格标准。这些标准的一些例子是一个人的一般健康状况或先前的治疗。

资格标准

适合学习的年龄

18年 至 80年 (成人、年长者)

接受健康志愿者

不

有资格学习的性别

全部

描述

Inclusion Criteria:

  • Subject has provided informed consent prior to initiation of any study-specific activities/procedures.
  • Male or female subject ≥ 18 years of age at the time of screening, with end stage renal disease receiving hemodialysis;
  • Body mass index is between 18 and 38 kg/m², inclusive;
  • Corrected calcium (calculated) level is > 8.3 mg/dL and intact parathyroid hormone (PTH) level is between 300 - 1200, inclusive; all other laboratory tests within clinically acceptable range to the investigator and sponsor at screening;
  • Female subjects must be of non-reproductive potential (ie, postmenopausal by history - no menses for 1 year and follicle-stimulating hormone (FSH) level consistent with postmenopausal status; OR history of hysterectomy; OR history of bilateral tubal ligation);
  • Negative screen for potential drugs of abuse at screening, unless positive result is expected based on approved concomitant medications;
  • Negative alcohol test at screening;
  • Subject has functioning permanent dialysis access via fistula, hemodialysis (HD) catheter, or arteriovenous (AV) graft;
  • Subject must be receiving hemodialysis 3 times weekly for at least 1 year prior to day -1 (or is confirmed to be anuric based on historical and clinical assessment if on hemodialysis for less than one year), and have adequate hemodialysis with a delivered Kt/V ≥ 1.2 or urea reduction ratio (URR) ≥ 65% within 4 weeks to screening. The subject's routine hemodialysis session must be of 3-4.5 hours in duration, inclusive;
  • Subject has stable dialysis prescription and this prescription is not anticipated to change significantly during the course of the study.

Exclusion Criteria:

  • Female subjects who are lactating/breastfeeding or who plan to breastfeed while on study through 3 months after receiving the dose of study drug;
  • Females with a positive pregnancy test at screening;
  • Positive for human immunodeficiency virus (HIV) at screening or known diagnosis of acquired immune deficiency syndrome (AIDS);
  • Positive Hepatitis B Surface Antigen (HepBsAg) at screening (indicative of chronic Hepatitis B);
  • Positive for Hepatitis C virus ribonucleic acid (RNA) by polymerase chain reaction (PCR) at screening (indicative of active hepatitis C - screening is generally done by hepatitis C antibody (HepCAb), followed by hepatitis C virus RNA by PCR if HepCAb is positive);
  • Previous administration of AMG 416;
  • Previous administration of any [¹⁴C] labeled drug substance within 1 year before study drug administration;
  • Subject has received cinacalcet within the 30 days prior to study drug administration (treatment with cinacalcet is prohibited during the study);
  • Subject has known sensitivity to any of the products or components to be administered during dosing;
  • Use of concomitant medication other than that used in the management of end stage renal disease and its expected comorbidities that could in the opinion of the investigator or Amgen medical monitor interfere with the safety of subjects or interpretation of study results;
  • Known illicit drug abuse within 12 months of day -1;
  • Unwilling or unable to limit alcohol consumption throughout the course of the study;
  • Alcohol is limited to no more than 2 units per day during the outpatient period of the study through completion of day 39. A standard unit is equivalent to 12 ounces of regular beer, 8-9 ounces of malt liquor, 5 ounces of wine, or 1.5 ounces of 80 proof distilled spirits;
  • Receiving or has received any investigational drug (or is currently using an investigational device) within the 30 days before receiving study drug, or at least 10 times the respective elimination half-life (whichever is longer);
  • Subject has lost 500 mL or more of blood or plasma within 8 weeks of study drug administration or during the study period;
  • Subjects with hemodynamic instability during hemodialysis;
  • Anticipated or scheduled kidney transplant during the study period
  • Subject has an unstable medical condition based on medical history, physical examination, and routine laboratory tests, or is otherwise unstable in the judgment of the Investigator;
  • Subject has an active infection at screening or day -1, or a history of any illness that, in the opinion of the Investigator, might confound the results of the study or pose additional risk to the subject;
  • History of malignancy (within 5 years before day -1) of any type, other than surgically excised non-melanomatous skin cancers;
  • Subject's 12-lead electrocardiogram (ECG) at screening suggests unstable arrhythmia or other cardiac abnormality that could place the subject at increased risk, based upon the Investigator's opinion
  • Subject has poorly controlled hypertension;
  • Subject has a history of symptomatic ventricular dysrhythmias or Torsades de Pointes;
  • Subject has a history within the past 6 months of angina pectoris with symptoms that occur at rest or minimal activity or a history of congestive heart failure (New York Heart Association Classification III or IV);
  • Subject has a history of myocardial infarction, coronary angioplasty, or coronary arterial bypass grafting within the past 6 months prior to screening;
  • Subject is receiving treatment for a seizure disorder or has a history of a seizure within the last 12 months prior to screening;
  • Subject has had major surgery (excluding minor surgery and hemodialysis access repair) within the last 8 weeks prior to screening;
  • Subject likely to not be available to complete all protocol-required study visits or procedures, and/or to comply with all required study procedures to the best of the subject and Investigator's knowledge;
  • History or evidence of any other clinically significant disorder, condition or disease that, in the opinion of the investigator or Amgen physician, if consulted, would pose a risk to subject safety or interfere with the study evaluation, procedures or completion.

学习计划

本节提供研究计划的详细信息,包括研究的设计方式和研究的衡量标准。

研究是如何设计的?

设计细节

  • 主要用途:基础科学
  • 分配:不适用
  • 介入模型:单组作业
  • 屏蔽:无(打开标签)

武器和干预

参与者组/臂
干预/治疗
实验性的:[¹⁴C]Etelcalcetide
Participants received a single dose of 10 mg radiolabelled etelcalcetide administered by intravenous (IV) bolus injection at the end of hemodialysis on day 1.
750 nCi of [¹⁴C]etelcalcetide formulated as a single 10 mg dose of etelcaletide in 2 mL liquid solution for bolus intravenous (IV) administration at the end of hemodialysis.
其他名称:
  • AMG 416
  • Parsabiv™

研究衡量的是什么?

主要结果指标

结果测量
措施说明
大体时间
Cumulative Excretion of Radioactivity
大体时间:Day 1 to day 176
The total radioactivity in excreta (urine and feces) or dialysate and dialysis membrane is expressed as a percentage of the total radioactive [¹⁴C] administered (dose). Total radioactive counts in dialysate, dialyzer, feces, and urine were determined by accelerator mass spectrometry (AMS). Radioactivity excreted during non-sampled days was estimated by interpolation and extrapolation of the measured data.
Day 1 to day 176
Time to Maximum Observed Concentration (Tmax) of [¹⁴C]Etelcalcetide-derived Radioactivity in Plasma
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Total radioactive counts in plasma was determined by accelerator mass spectrometry (AMS).
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Maximum Observed Concentration (Cmax) of [¹⁴C]Etelcalcetide-derived Radioactivity in Plasma
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Time to Last Observed Plasma Concentration of [¹⁴C]Etelcalcetide-derived Radioactivity in Plasma
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Last Observed Plasma Concentration (Clast) of [¹⁴C]Etelcalcetide-derived Radioactivity in Plasma
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Apparent Terminal Half-life (T½) of [¹⁴C]Etelcalcetide-derived Radioactivity in Plasma
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Area Under the Curve From Time Zero to 3 Days Post-dose (AUC3d) of [¹⁴C]Etelcalcetide-derived Radioactivity in Plasma
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Area Under the Curve From Time Zero to 10 Days Post-dose (AUC10d) of [¹⁴C]Etelcalcetide-derived Radioactivity in Plasma
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Area Under the Arterial Plasma Concentration-time Curve Obtained During Hemodialysis on Day 4 for Etelcalcetide
大体时间:Day 4 within 10 minutes after the start of hemodialysis, at 2 hours after the start of hemodialysis, and within 10 minutes before the end of hemodialysis.
Etelcalcetide plasma concentrations were determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS).
Day 4 within 10 minutes after the start of hemodialysis, at 2 hours after the start of hemodialysis, and within 10 minutes before the end of hemodialysis.
Area Under the Venous Plasma Concentration-time Curve Obtained During Hemodialysis on Day 4 for Etelcalcetide
大体时间:Day 4 within 10 minutes after the start of hemodialysis, at 2 hours after the start of hemodialysis, and within 10 minutes before the end of hemodialysis.
Etelcalcetide plasma concentrations were determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS).
Day 4 within 10 minutes after the start of hemodialysis, at 2 hours after the start of hemodialysis, and within 10 minutes before the end of hemodialysis.

次要结果测量

结果测量
措施说明
大体时间
Time to Maximum Observed Concentration (Tmax) of Etelcalcetide
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Etelcalcetide plasma concentrations were determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS).
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Maximum Observed Concentration (Cmax) of Etelcalcetide
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Time to Last Observed Plasma Concentration of Etelcalcetide
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Last Observed Plasma Concentration (Clast) of Etelcalcetide
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Area Under the Curve From Time Zero to 3 Days Post-dose (AUC3d) of Etelcalcetide
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Area Under the Curve From Time Zero to 10 Days Post-dose (AUC10d) of Etelcalcetide
大体时间:Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Samples were collected from pre-dose on day 1 to day 39; additional samples were collected at 3 consecutive hemodialysis sessions from days 129 -148 and approximately 1 month later at an additional 3 consecutive hemodialysis sessions from days 157-176.
Hemodialysis Clearance of Etelcalcetide During Hemodialysis on Day 4
大体时间:Day 4 within 10 minutes after the start of hemodialysis, at 2 hours after the start of hemodialysis, and within 10 minutes before the end of hemodialysis.
Day 4 within 10 minutes after the start of hemodialysis, at 2 hours after the start of hemodialysis, and within 10 minutes before the end of hemodialysis.
Hemodialysis Extraction Ratio for Etelcalcetide During Hemodialysis on Day 4
大体时间:Day 4 within 10 minutes after the start of hemodialysis, at 2 hours after the start of hemodialysis, and within 10 minutes before the end of hemodialysis.
Day 4 within 10 minutes after the start of hemodialysis, at 2 hours after the start of hemodialysis, and within 10 minutes before the end of hemodialysis.
Number of Participants With Adverse Events
大体时间:From first dose of etelcalcetide to day 39
A treatment-related adverse event (TRAE) is any adverse event (AE) that per investigator review has a reasonable possibility of being caused by the investigational product.
From first dose of etelcalcetide to day 39
Number of Participants With Anti-etelcalcetide Antibodies
大体时间:Day -1 and day 39
The presence of anti-etelcalcetide antibodies was assessed and confirmed using a dual-flow cell biosensor immunoassay at baseline (day -1) and at the end of study visit (day 39).
Day -1 and day 39

合作者和调查者

在这里您可以找到参与这项研究的人员和组织。

赞助

出版物和有用的链接

负责输入研究信息的人员自愿提供这些出版物。这些可能与研究有关。

研究记录日期

这些日期跟踪向 ClinicalTrials.gov 提交研究记录和摘要结果的进度。研究记录和报告的结果由国家医学图书馆 (NLM) 审查,以确保它们在发布到公共网站之前符合特定的质量控制标准。

研究主要日期

学习开始 (实际的)

2014年2月7日

初级完成 (实际的)

2014年4月15日

研究完成 (实际的)

2014年8月15日

研究注册日期

首次提交

2014年2月3日

首先提交符合 QC 标准的

2014年2月3日

首次发布 (估计)

2014年2月4日

研究记录更新

最后更新发布 (实际的)

2018年8月31日

上次提交的符合 QC 标准的更新

2018年8月2日

最后验证

2018年8月1日

更多信息

此信息直接从 clinicaltrials.gov 网站检索,没有任何更改。如果您有任何更改、删除或更新研究详细信息的请求,请联系 register@clinicaltrials.gov. clinicaltrials.gov 上实施更改,我们的网站上也会自动更新.

订阅