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

29 de septiembre de 2015 actualizado por: 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.

Descripción general del estudio

Estado

Terminado

Intervención / Tratamiento

Tipo de estudio

Intervencionista

Inscripción (Actual)

19

Fase

  • Fase 1

Contactos y Ubicaciones

Esta sección proporciona los datos de contacto de quienes realizan el estudio e información sobre dónde se lleva a cabo este estudio.

Ubicaciones de estudio

    • Florida
      • Miami, Florida, Estados Unidos, 33014
        • Otsuka Investigational Site
    • Minnesota
      • Minneapolis, Minnesota, Estados Unidos, 55404
        • Otsuka Investigational Site

Criterios de participación

Los investigadores buscan personas que se ajusten a una determinada descripción, denominada criterio de elegibilidad. Algunos ejemplos de estos criterios son el estado de salud general de una persona o tratamientos previos.

Criterio de elegibilidad

Edades elegibles para estudiar

18 años y mayores (Adulto, Adulto Mayor)

Acepta Voluntarios Saludables

Géneros elegibles para el estudio

Todos

Descripción

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).

Plan de estudios

Esta sección proporciona detalles del plan de estudio, incluido cómo está diseñado el estudio y qué mide el estudio.

¿Cómo está diseñado el estudio?

Detalles de diseño

  • Propósito principal: Tratamiento
  • Asignación: No aleatorizado
  • Modelo Intervencionista: Asignación paralela
  • Enmascaramiento: Ninguno (etiqueta abierta)

Armas e Intervenciones

Grupo de participantes/brazo
Intervención / Tratamiento
Comparador activo: Group 1
subjects with normal renal function
administered orally
Comparador activo: Group 2
severely renally impaired subjects
administered orally

¿Qué mide el estudio?

Medidas de resultado primarias

Medida de resultado
Medida Descripción
Periodo de tiempo
Unbound Area Under the Concentration (AUC) Time Curve Calculated to the Last Observable Concentration Brexpiprazole (AUCt,u).
Periodo de tiempo: 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).
Periodo de tiempo: 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).
Periodo de tiempo: 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

Medidas de resultado secundarias

Medida de resultado
Medida Descripción
Periodo de tiempo
AUC Time Curve of Brexpiprazole Metabolite (DM-3411) Calculated to the Last Observable Concentration at Time t (AUCt).
Periodo de tiempo: 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∞).
Periodo de tiempo: 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).
Periodo de tiempo: 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).
Periodo de tiempo: 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).
Periodo de tiempo: 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).
Periodo de tiempo: 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).
Periodo de tiempo: 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).
Periodo de tiempo: 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).
Periodo de tiempo: 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).
Periodo de tiempo: 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.
Periodo de tiempo: 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.

Colaboradores e Investigadores

Aquí es donde encontrará personas y organizaciones involucradas en este estudio.

Investigadores

  • Director de estudio: Aleksandar Skuban, Otsuka Pharmaceutical Development & Commercialization, Inc.

Fechas de registro del estudio

Estas fechas rastrean el progreso del registro del estudio y los envíos de resultados resumidos a ClinicalTrials.gov. Los registros del estudio y los resultados informados son revisados ​​por la Biblioteca Nacional de Medicina (NLM) para asegurarse de que cumplan con los estándares de control de calidad específicos antes de publicarlos en el sitio web público.

Fechas importantes del estudio

Inicio del estudio

1 de enero de 2011

Finalización primaria (Actual)

1 de diciembre de 2011

Finalización del estudio (Actual)

1 de enero de 2012

Fechas de registro del estudio

Enviado por primera vez

1 de febrero de 2011

Primero enviado que cumplió con los criterios de control de calidad

1 de febrero de 2011

Publicado por primera vez (Estimar)

3 de febrero de 2011

Actualizaciones de registros de estudio

Última actualización publicada (Estimar)

29 de octubre de 2015

Última actualización enviada que cumplió con los criterios de control de calidad

29 de septiembre de 2015

Última verificación

1 de septiembre de 2015

Más información

Términos relacionados con este estudio

Esta información se obtuvo directamente del sitio web clinicaltrials.gov sin cambios. Si tiene alguna solicitud para cambiar, eliminar o actualizar los detalles de su estudio, comuníquese con register@clinicaltrials.gov. Tan pronto como se implemente un cambio en clinicaltrials.gov, también se actualizará automáticamente en nuestro sitio web. .

Ensayos clínicos sobre OPC-34712

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