Evaluation Study of the Bioavailability of Brexpiprazole Orally Disintegrating Tablets in Healthy Male Subjects

A Single-center, Open-label, Randomized, Three-way, Crossover Trial to Evaluate the Bioavailability of Brexpiprazole (OPC-34712) Orally Disintegrating Tablets Relative to Brexpiprazole (OPC-34712) Conventional Tablets in Healthy Male Subjects

The ratios of the geometric means of the ODT formulation to those of the reference formulation (conventional tablet) for the bioavailability variables (Cmax, AUCt, and AUC∞ of brexpiprazole (OPC-34712)).

Study Overview

• Status: Completed
• Conditions: Healthy Adult Male
• Intervention / Treatment: Drug: OPC-34712

• Study Type: Interventional
• Enrollment (Actual): 18
• Phase: Phase 1

Contacts and Locations

Study Locations

• Japan
  • Kyusyu Region, Japan

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 16 years to 41 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Capable of providing written informed consent prior to initiation of any trial-related procedures, and able, in the opinion of the investigator, to comply with all requirements of the trial

Exclusion Criteria:

• Clinically significant abnormality at the time of screening (eg, significant deviation from reference ranges) or in medical history that, in the opinion of investigator or sponsor may place the subject at risk or interfere with outcome variables, including drug absorption, distribution, metabolism, and excretion
• History of serious mental disorder
• History of drug or alcohol abuse within 2 years prior to screening
• History of any significant drug allergy
• Use of an investigational drug within 120 days prior to the first dosing of trial drug
• Use of tobacco products or daily exposure to secondhand smoke within 2 months prior to screening
• Consumption of grapefruit, grapefruit products, Seville oranges, Seville orange products, starfruit, or starfruit products within 72 hours prior to dosing
• Use of prescription, over-the-counter, or herbal medication, vitamin supplements, or St. John's Wort within 14 days prior to the first dosing of trial drug, or of antibiotics within 30 days prior to the first dosing of trial drug
• History of major surgery of the digestive tract (excluding appendectomy)
• Any subject who, in the opinion of the investigator, should not participate in the trial

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Non-Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: OPC-34712 disintegrating tablet with water; OPC-34712 (4 mg) orally disintegrating tablet is administered with water.	Drug: OPC-34712; Other Names: Brexpiprazole
Experimental: OPC-34712 disintegrating tablet without water; OPC-34712 (4 mg) orally disintegrating tablet is administered without water.	Drug: OPC-34712; Other Names: Brexpiprazole
Experimental: OPC-34712 conventional tablet with water; OPC-34712 (4 mg) conventional tablet is administered with water.	Drug: OPC-34712; Other Names: Brexpiprazole

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Maximum Plasma Concentration (Cmax) of OPC-34712	To evaluate Cmax of OPC-34712 4-mg ODT formulation relative to 4-mg conventional tablet formulation	Predose, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 48, 72, 96, 120，144, 168, 216, 264, and 312 hours postdose
Area Under the Concentration-time Curve From Time Zero to Infinity (AUC∞) of OPC-34712	To evaluate AUC∞ of OPC-34712 4-mg ODT formulation relative to 4-mg conventional tablet formulation	Predose, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 48, 72, 96, 120，144, 168, 216, 264, and 312 hours postdose

Collaborators and Investigators

• Sponsor: Otsuka Pharmaceutical Co., Ltd.

Study record dates

Study Major Dates

• Study Start (Actual): September 27, 2016
• Primary Completion (Actual): November 27, 2016
• Study Completion (Actual): November 27, 2016

Study Registration Dates

• First Submitted: August 8, 2016
• First Submitted That Met QC Criteria: August 17, 2016
• First Posted (Estimate): August 23, 2016

Study Record Updates

• Last Update Posted (Actual): February 23, 2021
• Last Update Submitted That Met QC Criteria: February 3, 2021
• Last Verified: February 1, 2021

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Serotonin Agents; Dopamine Agonists; Dopamine Agents; Brexpiprazole
• Other Study ID Numbers: 331-102-00019; JapicCTI-163351 (Other Identifier: Japic)