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Trial Evaluating OPC-34712 in Subjects With Normal Renal Function and Renally Impaired Subjects

29 сентября 2015 г. обновлено: Otsuka Pharmaceutical Development & Commercialization, Inc.

A Single-dose, Open-label, Parallel-group, Matched Trial Evaluating the Pharmacokinetics of Oral OPC-34712 Tablets in Subjects With Normal Renal Function and Renally Impaired Subjects

This trial is an open-label, multi-center, parallel-arm, single-dose trial in 2 groups: 1 group of subjects with normal renal function and 1 group of severely renally impaired subjects.

Обзор исследования

Статус

Завершенный

Вмешательство/лечение

Тип исследования

Интервенционный

Регистрация (Действительный)

19

Фаза

  • Фаза 1

Контакты и местонахождение

В этом разделе приведены контактные данные лиц, проводящих исследование, и информация о том, где проводится это исследование.

Места учебы

    • Florida
      • Miami, Florida, Соединенные Штаты, 33014
        • Otsuka Investigational Site
    • Minnesota
      • Minneapolis, Minnesota, Соединенные Штаты, 55404
        • Otsuka Investigational Site

Критерии участия

Исследователи ищут людей, которые соответствуют определенному описанию, называемому критериям приемлемости. Некоторыми примерами этих критериев являются общее состояние здоровья человека или предшествующее лечение.

Критерии приемлемости

Возраст, подходящий для обучения

18 лет и старше (Взрослый, Пожилой взрослый)

Принимает здоровых добровольцев

Да

Полы, имеющие право на обучение

Все

Описание

Inclusion Criteria:

  • Male or female (non-childbearing potential) subjects ≥ 18 years of age.
  • Ability to provide written informed consent prior to initiation of any trial-related procedures, and ability, in the opinion of the principal investigator, to comply with all the requirements of the trial.
  • Male and female subjects who are surgically sterile; female subjects who have been postmenopausal for at least 12 consecutive months (confirmed by follicle stimulating hormone sample at Screening); or male subjects who agree to remain abstinent or to practice double-barrier forms of birth control and refrain from sperm donation from trial Screening through 90 days from the last dose of the investigational medicinal product.
  • Body weight within ± 35% of ideal body weight as defined in the 1983 Metropolitan Height and Weight Tables (see Appendix 4, Appendix 5, and Appendix 6). Minimum body weight no less than 50 kg.

Inclusion Criteria for Subjects with Normal Renal Function

  • Subjects who are in good health as determined by a medical history, physical examination, serum chemistry, hematology, urinalysis, hepatitis B and C tests, and human immunodeficiency virus (HIV) testing.
  • Creatinine clearance > 80 mL/min indicating normal renal function.

Inclusion Criteria for Renally Impaired Subjects

  • Renally impaired subjects may be taking medications which, in the opinion of the clinical investigator and sponsor, are believed to be therapeutic for the subjects (but do not affect OPC-34712 absorption, distribution, metabolism, or elimination). Inhibitors and inducers of CYP3A4 and inhibitors of CYP2D6 are not allowed.
  • Creatinine clearance < 30 mL/min indicating severe renal impairment.
  • Subjects with renal impairment should have relatively stable renal function as determined by creatinine clearance and otherwise be in generally good health.

Exclusion Criteria:

Clinically significant abnormality in past medical history, or at the screening physical examination, that in the investigator's or sponsor's opinion may place the subject at risk or interfere with outcome variables including absorption, distribution, metabolism, and excretion of drug.

  • Any surgical or medical condition (active or chronic) that may interfere with drug absorption, distribution, metabolism, or excretion, or any other condition that may place the subject at risk.
  • History of drug and/or alcohol abuse within 2 years prior to Screening.
  • A positive urine alcohol test and/or urine drug screen for substance of abuse at Screening or upon check-in to the trial site.
  • The donation of blood or plasma within 30 days prior to dosing.
  • Any history of significant bleeding or hemorrhagic tendencies.
  • History of or current hepatitis or carriers of hepatitis B surface antigen (HBsAg) and/or hepatitis C antibodies (anti-HCV).
  • History of acquired immunodeficiency syndrome or determined human immunodeficiency virus (HIV) positive at Screening.
  • Use of an investigational drug or product, or participation in a drug trial within 30 days prior to dosing.
  • Previous exposure to OPC-34712.
  • History of clinically significant drug allergies or sensitivities.
  • Subjects who are pregnant or breastfeeding. A negative serum pregnancy test must be confirmed prior to administration of trial medication for all female subjects.
  • Subjects who have a supine pulse rate, after resting for ≥ 3 minutes, outside the range of 40 to 90 bpm. The sponsor may allow exceptions if they are not deemed clinically significant.

Exclusion Criteria for Healthy Subjects

  • Clinically significant abnormal findings in the serum chemistry, hematology, or urinalysis results obtained at Screening or Day -1.
  • Use of prescription, over-the-counter, herbal medication or vitamin supplements within 14 days prior to dosing and antibiotics within 30 days prior to dosing. The sponsor may allow exceptions only if the medication's administration is deemed unlikely to impact the pharmacokinetic result. Inhibitors and inducers of CYP3A4 and inhibitors of CYP2D6 are not allowed.
  • Subjects who have supine, sitting, or standing blood pressure, after resting for ≥ 3 minutes, higher than 130/80 mmHg or lower than 100/50 mmHg. The sponsor may allow exceptions if they are not deemed clinically significant.

Exclusion Criteria for Renally Impaired Subjects

  • Subjects that have undergone a renal transplant.
  • Renally impaired subjects may be taking medications which, in the opinion of the clinical investigator and sponsor, are believed to be therapeutic for the subjects (but do not affect OPC-34712 absorption, distribution, metabolism, or elimination). Inhibitors and inducers of CYP3A4 and inhibitors of CYP2D6 are not allowed.
  • Clinically significant abnormal findings in the serum chemistry, hematology, or urinalysis results obtained at Screening or Day -1, other than those associated with underlying renal conditions and other stable medical conditions consistent with the disease processes.
  • Subject requiring dialysis or expected to require dialysis within 45 days.
  • Subjects who have supine, sitting, or standing blood pressure, after resting for ≥ 3 minutes, higher than 160/95 mmHg or lower than 100/50 mmHg. The sponsor may allow exceptions if they are not deemed clinically significant.
  • Subjects with evidence of delirium.
  • Clinically relevant changes on electrocardiogram such as any atrioventricular block, prolongation of the QRS complex over 120 msec (for both male and female subjects), or with a QTcF interval ≥ 450 msec.
  • Any subject who, in the opinion of the sponsor or the investigator, should not participate in the trial.
  • Consumption of alcohol and/or food and beverages containing methylxanthines, grapefruit, grapefruit juice, Seville oranges, or Seville orange juice within 72 hours prior to dosing.
  • Use of any drug known or suspected of inhibiting or stimulating hepatic drug metabolism enzymes within 30 days prior to Screening.
  • Exposure to any substances known to stimulate hepatic microsomal enzymes within 30 days prior to Screening through the end of the trial (eg, occupational exposure to pesticides, organic solvents).
  • History of serious mental disorders.
  • Major surgery of the digestive tract (excluding appendectomy).

Учебный план

В этом разделе представлена ​​подробная информация о плане исследования, в том числе о том, как планируется исследование и что оно измеряет.

Как устроено исследование?

Детали дизайна

  • Основная цель: Уход
  • Распределение: Нерандомизированный
  • Интервенционная модель: Параллельное назначение
  • Маскировка: Нет (открытая этикетка)

Оружие и интервенции

Группа участников / Армия
Вмешательство/лечение
Активный компаратор: Group 1
subjects with normal renal function
administered orally
Активный компаратор: Group 2
severely renally impaired subjects
administered orally

Что измеряет исследование?

Первичные показатели результатов

Мера результата
Мера Описание
Временное ограничение
Unbound Area Under the Concentration (AUC) Time Curve Calculated to the Last Observable Concentration Brexpiprazole (AUCt,u).
Временное ограничение: Day 1 to Day 8
Blood samples were collected on Day 1 at Predose (within 15 minutes of dosing) and at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours Postdose or at Early Termination (ET). Unbound fraction of drug in plasma was calculated as 100% - mean percent of brexpiprazole bound to plasma protein for each participant.
Day 1 to Day 8
Unbound Area Under AUC- Time Curve From Time Zero to Infinity (AUC∞,u).
Временное ограничение: Day 1 to Day 8
Blood samples were collected at Predose (within 15 minutes of dosing) and at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours or at ET. Unbound fraction of drug in plasma was calculated as 100% - mean percent of brexpiprazole bound to plasma protein for each participant.
Day 1 to Day 8
Unbound Maximum (Peak) Plasma Concentration of Brexpiprazole (Cmax,u).
Временное ограничение: Day 1 to Day 8
Blood samples were collected at Predose (within 15 minutes of dosing) and at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours or at ET. Unbound fraction of drug in plasma was calculated as 100% - mean percent of brexpiprazole bound to plasma protein for each participant.
Day 1 to Day 8

Вторичные показатели результатов

Мера результата
Мера Описание
Временное ограничение
AUC Time Curve of Brexpiprazole Metabolite (DM-3411) Calculated to the Last Observable Concentration at Time t (AUCt).
Временное ограничение: Day 1 to Day 8
Blood samples were collected at Predose (within 15 minutes of dosing) and at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours or at ET. The AUCt was estimated using the linear trapezoidal rule.
Day 1 to Day 8
AUC Time Curve of Brexpiprazole From Time Zero to Infinity (AUC∞).
Временное ограничение: Day 1 to Day 8
Blood samples were collected at Predose (within 15 minutes of dosing) and at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours or at ET. The AUC∞ was estimated using the linear trapezoidal rule.
Day 1 to Day 8
Maximum Plasma Concentration of Brexpiprazole Metabolite (DM-3411) (Cmax).
Временное ограничение: Day 1 to Day 8
Blood samples were collected at Predose (within 15 minutes of dosing) and at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours or at ET. Unbound fraction of drug in plasma was calculated as 100% - mean percent of brexpiprazole bound to plasma protein for each participant.
Day 1 to Day 8
Time to Cmax of Brexiprazole Metabolite (DM-3411) (Tmax).
Временное ограничение: Day 1 to Day 8
Blood samples were collected at Predose (within 15 minutes of dosing) and at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours or at ET. Tmax is the time taken to reach highest measured concentration of the drug during the dosing interval.
Day 1 to Day 8
Apparent Clearance From Plasma After Extravascular Administration of Brexpiprazole (CL/F).
Временное ограничение: Day 1 to Day 8
The value of CL/F was determined as Dose/AUC∞. Clearance of a drug was a measure of the rate at which a drug was metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) was influenced by the fraction of the dose absorbed. Clearance was estimated from population PK modeling. Drug clearance was a quantitative measure of the rate at which a drug substance was removed from the blood.
Day 1 to Day 8
Unbound Fraction of Brexpiprazole in Plasma (fu).
Временное ограничение: Day 1 to Day 8
Blood samples were collected at Predose (within 15 minutes of dosing) and at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours or at ET. Unbound fraction of drug in plasma was calculated as 100% - mean percent of brexpiprazole bound to plasma protein for each participant.
Day 1 to Day 8
Apparent Unbound Clearance From Plasma After Extravascular Administration of Brexpiprazole (CLu/F).
Временное ограничение: Day 1 to Day 8
Blood samples were collected at Predose (within 15 minutes of dosing) and at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours or at ET. Unbound fraction of drug in plasma was calculated as 100% - mean percent of brexpiprazole bound to plasma protein for each participant.
Day 1 to Day 8
Terminal-phase Elimination Half-life of Brexpiprazole (t1/2,z).
Временное ограничение: Day 1 to Day 8
Blood samples were collected at Predose (within 15 minutes of dosing) and at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, and 168 hours or at ET. Unbound fraction of drug in plasma was calculated as 100% - mean percent of brexpiprazole bound to plasma protein for each participant.
Day 1 to Day 8
Renal Clearance (CLr) of Brexipiprazole Metabolite (DM-3411).
Временное ограничение: Day 1 to Day 8
Urine samples were collected at Predose at intervals of 0 to 24, 24 to 48, 48 to 72, 72 to 96, 96 to 120, 120 to 144, and 144 to 168 hours postdose. Unbound fraction of drug in plasma was calculated as 100% - mean percent of brexpiprazole bound to plasma protein for each participant.
Day 1 to Day 8
Fraction of the Systemically Available Brexpiprazole Metabolite (DM-3411) Excreted Into the Urine (fe,u).
Временное ограничение: Day 1 to Day 8
Urine samples were collected at Predose and at intervals of 0 to 24, 24 to 48, 48 to 72, 72 to 96, 96 to 120, 120 to 144, and 144 to 168 hours postdose. Unbound fraction of drug in plasma was calculated as 100% - mean percent of brexpiprazole bound to plasma protein for each participant.
Day 1 to Day 8
The Abnormalities Found in Vital Signs, ECGs, and Clinical Laboratory Tests Are Reported as AEs Upon Study Physicians Discretion.
Временное ограничение: AEs were recorded from Screening (ICF was signed) to Follow-up 31 (+ 2) days.
An adverse event (AE) was an exacerbation of an existing problem or any new problem, experienced by a participant when enrolled in a trial, whether or not it was considered drug related by the study physician.
AEs were recorded from Screening (ICF was signed) to Follow-up 31 (+ 2) days.

Соавторы и исследователи

Здесь вы найдете людей и организации, участвующие в этом исследовании.

Следователи

  • Директор по исследованиям: Aleksandar Skuban, Otsuka Pharmaceutical Development & Commercialization, Inc.

Даты записи исследования

Эти даты отслеживают ход отправки отчетов об исследованиях и сводных результатов на сайт ClinicalTrials.gov. Записи исследований и сообщаемые результаты проверяются Национальной медицинской библиотекой (NLM), чтобы убедиться, что они соответствуют определенным стандартам контроля качества, прежде чем публиковать их на общедоступном веб-сайте.

Изучение основных дат

Начало исследования

1 января 2011 г.

Первичное завершение (Действительный)

1 декабря 2011 г.

Завершение исследования (Действительный)

1 января 2012 г.

Даты регистрации исследования

Первый отправленный

1 февраля 2011 г.

Впервые представлено, что соответствует критериям контроля качества

1 февраля 2011 г.

Первый опубликованный (Оценивать)

3 февраля 2011 г.

Обновления учебных записей

Последнее опубликованное обновление (Оценивать)

29 октября 2015 г.

Последнее отправленное обновление, отвечающее критериям контроля качества

29 сентября 2015 г.

Последняя проверка

1 сентября 2015 г.

Дополнительная информация

Термины, связанные с этим исследованием

Эта информация была получена непосредственно с веб-сайта clinicaltrials.gov без каких-либо изменений. Если у вас есть запросы на изменение, удаление или обновление сведений об исследовании, обращайтесь по адресу register@clinicaltrials.gov. Как только изменение будет реализовано на clinicaltrials.gov, оно будет автоматически обновлено и на нашем веб-сайте. .

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