Trial Outcomes & Findings for Bioequivalence Between Single Administration of ASC-01 (Aripiprazole/Sertraline Combination Drug) and Concomitant Single Administration of Aripiprazole and Sertraline, and Food Effect on Pharmacokinetics of ASC-01 in Healthy Male Adults (NCT NCT03342963)
NCT ID: NCT03342963
Last Updated: 2021-05-03
Results Overview
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
74 participants
Primary outcome timeframe
Baseline, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72,96, 144 and 168h after dosing
Results posted on
2021-05-03
Participant Flow
Participant milestones
| Measure |
Cohort 1: ASC-01 First
At Day 1 in Period I, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
At Day 1 in Period II, Aripiprazole 3 mg and sertraline 100 mg was administered after 10 or more hours of fasting.
There was a washout period of at least 35 days between Period I and Period II.
|
Cohort 1: Aripiprazole/Sertraline Concomitant First
At Day 1 in Period I, Aripiprazole 3 mg and sertraline 100 mg was administered after 10 or more hours of fasting.
At Day 1 in Period II, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
There was a washout period of at least 35 days between Period I and Period II.
|
Cohort 2: ASC-01 Under Fasted First
At Day 1 in Period I, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
At Day 1 in Period II, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered 30 minutes after the start of breakfast.
There was a washout period of at least 35 days between Period I and Period II.
|
Cohort 2: ASC-01 Under Fed First
At Day 1 in Period I, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered 30 minutes after the start of breakfast.
At Day 1 in Period II, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
There was a washout period of at least 35 days between Period I and Period II.
|
|---|---|---|---|---|
|
Overall Study
STARTED
|
27
|
27
|
10
|
10
|
|
Overall Study
COMPLETED
|
25
|
25
|
10
|
10
|
|
Overall Study
NOT COMPLETED
|
2
|
2
|
0
|
0
|
Reasons for withdrawal
| Measure |
Cohort 1: ASC-01 First
At Day 1 in Period I, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
At Day 1 in Period II, Aripiprazole 3 mg and sertraline 100 mg was administered after 10 or more hours of fasting.
There was a washout period of at least 35 days between Period I and Period II.
|
Cohort 1: Aripiprazole/Sertraline Concomitant First
At Day 1 in Period I, Aripiprazole 3 mg and sertraline 100 mg was administered after 10 or more hours of fasting.
At Day 1 in Period II, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
There was a washout period of at least 35 days between Period I and Period II.
|
Cohort 2: ASC-01 Under Fasted First
At Day 1 in Period I, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
At Day 1 in Period II, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered 30 minutes after the start of breakfast.
There was a washout period of at least 35 days between Period I and Period II.
|
Cohort 2: ASC-01 Under Fed First
At Day 1 in Period I, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered 30 minutes after the start of breakfast.
At Day 1 in Period II, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
There was a washout period of at least 35 days between Period I and Period II.
|
|---|---|---|---|---|
|
Overall Study
Adverse Event
|
1
|
2
|
0
|
0
|
|
Overall Study
Withdrawal by Subject
|
1
|
0
|
0
|
0
|
Baseline Characteristics
Bioequivalence Between Single Administration of ASC-01 (Aripiprazole/Sertraline Combination Drug) and Concomitant Single Administration of Aripiprazole and Sertraline, and Food Effect on Pharmacokinetics of ASC-01 in Healthy Male Adults
Baseline characteristics by cohort
| Measure |
Cohort 1: ASC-01 First
n=27 Participants
At Day 1 in Period I, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
At Day 1 in Period II, Aripiprazole 3 mg and sertraline 100 mg was administered after 10 or more hours of fasting.
There was a washout period of at least 35 days between Period I and Period II.
|
Cohort 1: Aripiprazole/Sertraline Concomitant First
n=27 Participants
At Day 1 in Period I, Aripiprazole 3 mg and sertraline 100 mg was administered after 10 or more hours of fasting.
At Day 1 in Period II, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
There was a washout period of at least 35 days between Period I and Period II.
|
Cohort 2: ASC-01 Under Fasted First
n=10 Participants
At Day 1 in Period I, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
At Day 1 in Period II, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered 30 minutes after the start of breakfast.
There was a washout period of at least 35 days between Period I and Period II.
|
Cohort 2: ASC-01 Under Fed First
n=10 Participants
At Day 1 in Period I, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered 30 minutes after the start of breakfast.
At Day 1 in Period II, ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
There was a washout period of at least 35 days between Period I and Period II.
|
Total
n=74 Participants
Total of all reporting groups
|
|---|---|---|---|---|---|
|
Age, Categorical
<=18 years
|
0 Participants
n=99 Participants
|
0 Participants
n=107 Participants
|
0 Participants
n=206 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=31 Participants
|
|
Age, Categorical
Between 18 and 65 years
|
27 Participants
n=99 Participants
|
27 Participants
n=107 Participants
|
10 Participants
n=206 Participants
|
10 Participants
n=7 Participants
|
74 Participants
n=31 Participants
|
|
Age, Categorical
>=65 years
|
0 Participants
n=99 Participants
|
0 Participants
n=107 Participants
|
0 Participants
n=206 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=31 Participants
|
|
Sex: Female, Male
Female
|
0 Participants
n=99 Participants
|
0 Participants
n=107 Participants
|
0 Participants
n=206 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=31 Participants
|
|
Sex: Female, Male
Male
|
27 Participants
n=99 Participants
|
27 Participants
n=107 Participants
|
10 Participants
n=206 Participants
|
10 Participants
n=7 Participants
|
74 Participants
n=31 Participants
|
|
Race/Ethnicity, Customized
Japanese
|
27 Participants
n=99 Participants
|
27 Participants
n=107 Participants
|
10 Participants
n=206 Participants
|
10 Participants
n=7 Participants
|
74 Participants
n=31 Participants
|
|
Region of Enrollment
Japan
|
27 Participants
n=99 Participants
|
27 Participants
n=107 Participants
|
10 Participants
n=206 Participants
|
10 Participants
n=7 Participants
|
74 Participants
n=31 Participants
|
PRIMARY outcome
Timeframe: Baseline, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72,96, 144 and 168h after dosingPopulation: Pharmacokinetic Analysis Set comprised subjects who received IMP and for whom plasma drug concentration data were obtained.
Outcome measures
| Measure |
ASC-01
n=40 Participants
ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
|
Aripiprazole/Sertraline Concomitant
n=39 Participants
Aripiprazole 3 mg and sertraline 100 mg was administered after 10 or more hours of fasting.
|
|---|---|---|
|
Peak Plasma Concentration (Cmax) of Aripiprazole in Cohort 1
|
18.8 ng/mL
Standard Deviation 5.33
|
16.9 ng/mL
Standard Deviation 4.38
|
PRIMARY outcome
Timeframe: Baseline, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72,96, 144 and 168h after dosingPopulation: Pharmacokinetic Analysis Set comprised subjects who received IMP and for whom plasma drug concentration data were obtained.
Outcome measures
| Measure |
ASC-01
n=40 Participants
ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
|
Aripiprazole/Sertraline Concomitant
n=39 Participants
Aripiprazole 3 mg and sertraline 100 mg was administered after 10 or more hours of fasting.
|
|---|---|---|
|
Area Under the Plasma Concentration Versus Time Curve 168h (AUC168h) of Aripiprazole in Cohort 1
|
783 ng*h/mL
Standard Deviation 273
|
779 ng*h/mL
Standard Deviation 236
|
PRIMARY outcome
Timeframe: Baseline, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72,96, 144 and 168h after dosingPopulation: Pharmacokinetic Analysis Set comprised subjects who received IMP and for whom plasma drug concentration data were obtained.
Outcome measures
| Measure |
ASC-01
n=20 Participants
ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
|
Aripiprazole/Sertraline Concomitant
n=20 Participants
Aripiprazole 3 mg and sertraline 100 mg was administered after 10 or more hours of fasting.
|
|---|---|---|
|
Cmax of Aripiprazole and Sertraline in Cohort 2
Aripiprazole
|
16.9 ng/mL
Standard Deviation 5.23
|
16.6 ng/mL
Standard Deviation 3.74
|
|
Cmax of Aripiprazole and Sertraline in Cohort 2
Sertraline
|
28.9 ng/mL
Standard Deviation 10.7
|
36.5 ng/mL
Standard Deviation 15.6
|
PRIMARY outcome
Timeframe: Baseline, 1, 2, 3, 4, 5, 6, 8, 12, 24, 48, 72,96, 144 and 168h after dosingPopulation: Pharmacokinetic Analysis Set comprised subjects who received IMP and for whom plasma drug concentration data were obtained.
Outcome measures
| Measure |
ASC-01
n=20 Participants
ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
|
Aripiprazole/Sertraline Concomitant
n=20 Participants
Aripiprazole 3 mg and sertraline 100 mg was administered after 10 or more hours of fasting.
|
|---|---|---|
|
AUC168h of Aripiprazole and Sertraline in Cohort 2
Aripiprazole
|
701 ng*h/mL
Standard Deviation 221
|
865 ng*h/mL
Standard Deviation 219
|
|
AUC168h of Aripiprazole and Sertraline in Cohort 2
Sertraline
|
904 ng*h/mL
Standard Deviation 415
|
1060 ng*h/mL
Standard Deviation 468
|
Adverse Events
Cohort 1 - ASC-01
Serious events: 0 serious events
Other events: 44 other events
Deaths: 0 deaths
Cohort 1 - Aripiprazole/Sertraline Concomitant
Serious events: 0 serious events
Other events: 43 other events
Deaths: 0 deaths
Cohort 2 - ASC-01 Under Fasted
Serious events: 0 serious events
Other events: 12 other events
Deaths: 0 deaths
Cohort 2 - ASC-01 Under Fed
Serious events: 0 serious events
Other events: 14 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Cohort 1 - ASC-01
n=52 participants at risk
ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
|
Cohort 1 - Aripiprazole/Sertraline Concomitant
n=52 participants at risk
Aripiprazole 3 mg and sertraline 100 mg was administered after 10 or more hours of fasting.
|
Cohort 2 - ASC-01 Under Fasted
n=20 participants at risk
ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered after 10 or more hours of fasting.
|
Cohort 2 - ASC-01 Under Fed
n=20 participants at risk
ASC-01 (aripiprazole 3 mg/sertraline 100 mg combination drug) was administered 30 minutes after the start of breakfast.
|
|---|---|---|---|---|
|
Cardiac disorders
Tachycardia
|
5.8%
3/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
3.8%
2/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
|
Gastrointestinal disorders
Diarrhoea
|
13.5%
7/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
17.3%
9/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
15.0%
3/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
5.0%
1/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
|
Gastrointestinal disorders
Nausea
|
75.0%
39/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
73.1%
38/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
55.0%
11/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
50.0%
10/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
|
Gastrointestinal disorders
Vomiting
|
38.5%
20/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
32.7%
17/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
30.0%
6/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
45.0%
9/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
|
Infections and infestations
Pharyngitis
|
0.00%
0/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
1.9%
1/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
|
Infections and infestations
Nasopharyngitis
|
0.00%
0/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
5.0%
1/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
|
Investigations
Blood creatine phosphokinase increased
|
1.9%
1/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
1.9%
1/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
|
Metabolism and nutrition disorders
Decreased appetite
|
7.7%
4/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
5.8%
3/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
5.0%
1/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
5.0%
1/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
|
Nervous system disorders
Dizziness postural
|
0.00%
0/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
1.9%
1/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
10.0%
2/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
|
Nervous system disorders
Headache
|
0.00%
0/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
1.9%
1/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
|
Vascular disorders
Orthostatic hypotension
|
0.00%
0/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/52 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
0.00%
0/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
5.0%
1/20 • Treatment-emergent adverse events occurring up to 8 days after dosing date were collected.
Safety Set comprised subjects who received IMP at least once.
|
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