Trial Outcomes & Findings for Bioequivalence Study of Brexpiprazole Orally Disintegrating Tablets (ODT) 2mg (NCT NCT03902574)
NCT ID: NCT03902574
Last Updated: 2021-07-20
Results Overview
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
21 participants
Primary outcome timeframe
Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12,16, 24, 48, 72, 96, 120, 144, 168, 216, 264 and 312 hours postdose
Results posted on
2021-07-20
Participant Flow
Participant milestones
| Measure |
Sequence 1: ODT Without Water/Conventional/ODT With Water
Subjects randomized to Sequence 1 received a brexpiprazole ODT 2 mg without water on Day 1 in Period 1 (Days 1 to 20), then a brexpiprazole conventional tablet 2 mg on Day 21 in Period 2 (Days 21 to 40), then a brexpiprazole ODT 2 mg with water on Day 41 in Period 3 (Days 41 to 60).
|
Sequence 2: ODT With Water/ODT Without Water/Conventional
Subjects randomized to Sequence 2 received a brexpiprazole ODT 2 mg with water on Day 1 in Period 1 (Days 1 to 20), then a brexpiprazole ODT 2 mg without water on Day 21 in Period 2 (Days 21 to 40), then a brexpiprazole conventional tablet 2 mg on Day 41 in Period 3 (Days 41 to 60).
|
Sequence 3: Conventional/ODT With Water/ODT Without Water
Subjects randomized to Sequence 3 received a brexpiprazole conventional tablet 2 mg on Day 1 in Period 1 (Days 1 to 20), then a brexpiprazole ODT 2 mg with water on Day 21 in Period 2 (Days 21 to 40), then a brexpiprazole ODT 2 mg without water on Day 41 in Period 3 (Days 41 to 60).
|
|---|---|---|---|
|
Overall Study
STARTED
|
7
|
7
|
7
|
|
Overall Study
COMPLETED
|
7
|
7
|
6
|
|
Overall Study
NOT COMPLETED
|
0
|
0
|
1
|
Reasons for withdrawal
| Measure |
Sequence 1: ODT Without Water/Conventional/ODT With Water
Subjects randomized to Sequence 1 received a brexpiprazole ODT 2 mg without water on Day 1 in Period 1 (Days 1 to 20), then a brexpiprazole conventional tablet 2 mg on Day 21 in Period 2 (Days 21 to 40), then a brexpiprazole ODT 2 mg with water on Day 41 in Period 3 (Days 41 to 60).
|
Sequence 2: ODT With Water/ODT Without Water/Conventional
Subjects randomized to Sequence 2 received a brexpiprazole ODT 2 mg with water on Day 1 in Period 1 (Days 1 to 20), then a brexpiprazole ODT 2 mg without water on Day 21 in Period 2 (Days 21 to 40), then a brexpiprazole conventional tablet 2 mg on Day 41 in Period 3 (Days 41 to 60).
|
Sequence 3: Conventional/ODT With Water/ODT Without Water
Subjects randomized to Sequence 3 received a brexpiprazole conventional tablet 2 mg on Day 1 in Period 1 (Days 1 to 20), then a brexpiprazole ODT 2 mg with water on Day 21 in Period 2 (Days 21 to 40), then a brexpiprazole ODT 2 mg without water on Day 41 in Period 3 (Days 41 to 60).
|
|---|---|---|---|
|
Overall Study
Urinary drug test was positive on Day 20
|
0
|
0
|
1
|
Baseline Characteristics
Bioequivalence Study of Brexpiprazole Orally Disintegrating Tablets (ODT) 2mg
Baseline characteristics by cohort
| Measure |
Sequence 1: ODT Without Water/Conventional/ODT With Water
n=7 Participants
Subjects randomized to Sequence 1 received a brexpiprazole ODT 2 mg without water on Day 1 in Period 1 (Days 1 to 20), then a brexpiprazole conventional tablet 2 mg on Day 21 in Period 2 (Days 21 to 40), then a brexpiprazole ODT 2 mg with water on Day 41 in Period 3 (Days 41 to 60).
|
Sequence 2: ODT With Water/ODT Without Water/Conventional
n=7 Participants
Subjects randomized to Sequence 2 received a brexpiprazole ODT 2 mg with water on Day 1 in Period 1 (Days 1 to 20), then a brexpiprazole ODT 2 mg without water on Day 21 in Period 2 (Days 21 to 40), then a brexpiprazole conventional tablet 2 mg on Day 41 in Period 3 (Days 41 to 60).
|
Sequence 3: Conventional/ODT With Water/ODT Without Water
n=7 Participants
Subjects randomized to Sequence 3 received a brexpiprazole conventional tablet 2 mg on Day 1 in Period 1 (Days 1 to 20), then a brexpiprazole ODT 2 mg with water on Day 21 in Period 2 (Days 21 to 40), then a brexpiprazole ODT 2 mg without water on Day 41 in Period 3 (Days 41 to 60).
|
Total
n=21 Participants
Total of all reporting groups
|
|---|---|---|---|---|
|
Age, Continuous
|
28.1 years
STANDARD_DEVIATION 6.6 • n=5 Participants
|
27.1 years
STANDARD_DEVIATION 5.4 • n=7 Participants
|
28.9 years
STANDARD_DEVIATION 5.4 • n=5 Participants
|
28.0 years
STANDARD_DEVIATION 5.6 • n=4 Participants
|
|
Sex: Female, Male
Female
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
|
Sex: Female, Male
Male
|
7 Participants
n=5 Participants
|
7 Participants
n=7 Participants
|
7 Participants
n=5 Participants
|
21 Participants
n=4 Participants
|
|
Race/Ethnicity, Customized
Asian
|
7 Participants
n=5 Participants
|
7 Participants
n=7 Participants
|
7 Participants
n=5 Participants
|
21 Participants
n=4 Participants
|
|
Region of Enrollment
Japan
|
7 Participants
n=5 Participants
|
7 Participants
n=7 Participants
|
7 Participants
n=5 Participants
|
21 Participants
n=4 Participants
|
PRIMARY outcome
Timeframe: Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12,16, 24, 48, 72, 96, 120, 144, 168, 216, 264 and 312 hours postdosePopulation: Bioequivalence analysis set: subjects for whom the relevant bioequivalence variables are available for all periods
Outcome measures
| Measure |
Conventional Tablet
n=19 Participants
Brexpiprazole conventional tablet 2 mg was administered with water.
|
ODT Without Water
n=19 Participants
Brexpiprazole ODT 2 mg was administered without water.
|
ODT With Water
n=19 Participants
Brexpiprazole ODT 2 mg was administered with water.
|
|---|---|---|---|
|
Maximum (Peak) Plasma Concentration (Cmax) of Brexpiprazole
|
23.31 ng/mL
Standard Deviation 4.722
|
24.24 ng/mL
Standard Deviation 6.090
|
23.75 ng/mL
Standard Deviation 5.320
|
PRIMARY outcome
Timeframe: Pre-dose, 1, 2, 3, 4, 5, 6, 8, 12,16, 24, 48, 72, 96, 120, 144, 168, 216, 264, and 312 hours postdosePopulation: Bioequivalence analysis set: subjects for whom the relevant bioequivalence variables are available for all periods
Outcome measures
| Measure |
Conventional Tablet
n=19 Participants
Brexpiprazole conventional tablet 2 mg was administered with water.
|
ODT Without Water
n=19 Participants
Brexpiprazole ODT 2 mg was administered without water.
|
ODT With Water
n=19 Participants
Brexpiprazole ODT 2 mg was administered with water.
|
|---|---|---|---|
|
Area Under the Concentration-time Curve Calculated to the Last Observable Concentration at Time t (AUCt) of Brexpiprazole
|
1250 ng*h/mL
Standard Deviation 592
|
1340 ng*h/mL
Standard Deviation 629
|
1260 ng*h/mL
Standard Deviation 615
|
Adverse Events
Conventional Tablet
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
ODT Without Water
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
ODT With Water
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Conventional Tablet
n=21 participants at risk
Brexpiprazole conventional tablet 2 mg was administered with water.
|
ODT Without Water
n=20 participants at risk
Brexpiprazole ODT 2 mg was administered without water.
|
ODT With Water
n=20 participants at risk
Brexpiprazole ODT 2 mg was administered with water.
|
|---|---|---|---|
|
Gastrointestinal disorders
Nausea
|
4.8%
1/21 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
10.0%
2/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
|
Gastrointestinal disorders
Vomiting
|
4.8%
1/21 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
|
General disorders
Feeling Abnormal
|
4.8%
1/21 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
|
Hepatobiliary disorders
Hepatic Function Abnormal
|
4.8%
1/21 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
|
Infections and infestations
Gingivitis
|
0.00%
0/21 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
5.0%
1/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
|
Injury, poisoning and procedural complications
Contusion
|
4.8%
1/21 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
|
Investigations
Blood Urine Present
|
0.00%
0/21 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
5.0%
1/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
|
Nervous system disorders
Dizziness Postural
|
4.8%
1/21 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
5.0%
1/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
5.0%
1/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
|
Skin and subcutaneous tissue disorders
Rash
|
0.00%
0/21 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
0.00%
0/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
5.0%
1/20 • Treatment-emergent adverse events were collected from the start of IMP administration up to 63 days
The safety analysis set consisted of all randomized subjects who received at least one dose of IMP. All the 21 subjects randomized to treatment sequences were included in the safety analysis set. (The number of subjects who received conventional tablet, ODT without water, and ODT with water were 21, 20, and 20, respectively).
|
Additional Information
Director of Clinical Trials
Otsuka Pharmaceutical Co., LTD.
Phone: +81-3-6361-7366
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place