Trial Outcomes & Findings for Pharmacokinetic Interaction Between BIA 9-1067 and Standard-release Levodopa/Carbidopa (NCT NCT01533077)
NCT ID: NCT01533077
Last Updated: 2015-12-22
Results Overview
Mean pharmacokinetic parameters of L-beta-3,4-dihydroxyphenylalanine (levodopa) (L-DOPA)
COMPLETED
PHASE1
18 participants
pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.
2015-12-22
Participant Flow
Participant milestones
| Measure |
Group 1
Period 1: BIA 9-1067 50 mg Period 2: Sinemet® 100/25 1 h after the BIA 9-1067 50 mg Period 3: BIA 9-1067 50 mg + Sinemet® 100/25 Period 4: Sinemet® 100/25
BIA 9-1067: 50 mg of BIA 9-1067 (single-dose)
Sinemet® 100/25 mg: immediate-release levodopa/carbidopa 100/25 (single-dose).
|
Group 2
Period 1: Sinemet® 100/25 Period 2: BIA 9-1067 50 mg Period 3: Sinemet® 100/25 1 h after the BIA 9-1067 50 mg Period 4: BIA 9-1067 50 mg + Sinemet® 100/25
BIA 9-1067: 50 mg of BIA 9-1067 (single-dose)
Sinemet® 100/25 mg: immediate-release levodopa/carbidopa 100/25 (single-dose).
|
Group 3
Period 1: BIA 9-1067 50 mg + Sinemet® 100/25 Period 2: Sinemet® 100/25 Period 3: BIA 9-1067 50 mg Period 4: Sinemet® 100/25 1 h after the BIA 9-1067 50 mg
BIA 9-1067: 50 mg of BIA 9-1067 (single-dose)
Sinemet® 100/25 mg: immediate-release levodopa/carbidopa 100/25 (single-dose).
|
Group 4
Period 1: Sinemet® 100/25 1 h after the BIA 9-1067 50 mg Period 2: BIA 9-1067 50 mg + Sinemet® 100/25 Period 3: Sinemet® 100/25 Period 4: BIA 9-1067 50 mg
BIA 9-1067: 50 mg of BIA 9-1067 (single-dose)
Sinemet® 100/25 mg: immediate-release levodopa/carbidopa 100/25 (single-dose).
|
|---|---|---|---|---|
|
Overall Study
STARTED
|
5
|
5
|
4
|
4
|
|
Overall Study
BIA 9-1067 50 mg
|
5
|
5
|
4
|
4
|
|
Overall Study
Sinemet® 100/25
|
4
|
5
|
4
|
4
|
|
Overall Study
BIA 9-1067 50 mg + Sinemet® 100/25
|
4
|
4
|
4
|
4
|
|
Overall Study
Sinemet® 100/25 1 h After the BIA 9-1067
|
5
|
5
|
4
|
4
|
|
Overall Study
COMPLETED
|
4
|
4
|
4
|
4
|
|
Overall Study
NOT COMPLETED
|
1
|
1
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
Pharmacokinetic Interaction Between BIA 9-1067 and Standard-release Levodopa/Carbidopa
Baseline characteristics by cohort
| Measure |
Group 1
n=5 Participants
Period 1: BIA 9-1067 50 mg Period 2: Sinemet® 100/25 1 h after the BIA 9-1067 50 mg Period 3: BIA 9-1067 50 mg + Sinemet® 100/25 Period 4: Sinemet® 100/25
BIA 9-1067: 50 mg of BIA 9-1067 (single-dose)
Sinemet® 100/25 mg: immediate-release levodopa/carbidopa 100/25 (single-dose).
|
Group 2
n=5 Participants
Period 1: Sinemet® 100/25 Period 2: BIA 9-1067 50 mg Period 3: Sinemet® 100/25 1 h after the BIA 9-1067 50 mg Period 4: BIA 9-1067 50 mg + Sinemet® 100/25
BIA 9-1067: 50 mg of BIA 9-1067 (single-dose)
Sinemet® 100/25 mg: immediate-release levodopa/carbidopa 100/25 (single-dose).
|
Group 3
n=4 Participants
Period 1: BIA 9-1067 50 mg + Sinemet® 100/25 Period 2: Sinemet® 100/25 Period 3: BIA 9-1067 50 mg Period 4: Sinemet® 100/25 1 h after the BIA 9-1067 50 mg
BIA 9-1067: 50 mg of BIA 9-1067 (single-dose)
Sinemet® 100/25 mg: immediate-release levodopa/carbidopa 100/25 (single-dose).
|
Group 4
n=4 Participants
Period 1: Sinemet® 100/25 1 h after the BIA 9-1067 50 mg Period 2: BIA 9-1067 50 mg + Sinemet® 100/25 Period 3: Sinemet® 100/25 Period 4: BIA 9-1067 50 mg
BIA 9-1067: 50 mg of BIA 9-1067 (single-dose)
Sinemet® 100/25 mg: immediate-release levodopa/carbidopa 100/25 (single-dose).
|
Total
n=18 Participants
Total of all reporting groups
|
|---|---|---|---|---|---|
|
Age, Categorical
<=18 years
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
|
Age, Categorical
Between 18 and 65 years
|
5 Participants
n=5 Participants
|
5 Participants
n=7 Participants
|
4 Participants
n=5 Participants
|
4 Participants
n=4 Participants
|
18 Participants
n=21 Participants
|
|
Age, Categorical
>=65 years
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=21 Participants
|
|
Sex: Female, Male
Female
|
2 Participants
n=5 Participants
|
2 Participants
n=7 Participants
|
2 Participants
n=5 Participants
|
2 Participants
n=4 Participants
|
8 Participants
n=21 Participants
|
|
Sex: Female, Male
Male
|
3 Participants
n=5 Participants
|
3 Participants
n=7 Participants
|
2 Participants
n=5 Participants
|
2 Participants
n=4 Participants
|
10 Participants
n=21 Participants
|
PRIMARY outcome
Timeframe: pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Mean pharmacokinetic parameters of L-beta-3,4-dihydroxyphenylalanine (levodopa) (L-DOPA)
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
Cmax - Maximum Observed Plasma Concentration (L-DOPA)
|
1070 ng/mL
Standard Deviation 328
|
1105 ng/mL
Standard Deviation 363
|
1198 ng/mL
Standard Deviation 294
|
PRIMARY outcome
Timeframe: pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Pharmacokinetic parameters of L-beta-3,4-dihydroxyphenylalanine (levodopa) (L-DOPA). For tmax = time to Cmax values are presented as median with range values.
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
Tmax - Time of Occurrence of Cmax Maximum Observed Plasma Concentration (L-DOPA)
|
1.0 hours
Interval 0.5 to 2.0
|
1.0 hours
Interval 0.5 to 4.0
|
0.5 hours
Interval 0.5 to 1.0
|
PRIMARY outcome
Timeframe: pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Mean pharmacokinetic parameters of L-beta-3,4-dihydroxyphenylalanine (levodopa) (L-DOPA)
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
AUC0-t - Area Under the Plasma Concentration-time Curve to Last Measurable Time Point (L-DOPA)
|
2289 ng.h/mL
Standard Deviation 729
|
2611 ng.h/mL
Standard Deviation 916
|
2459 ng.h/mL
Standard Deviation 825
|
PRIMARY outcome
Timeframe: pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Mean pharmacokinetic parameters of L-beta-3,4-dihydroxyphenylalanine (levodopa) (L-DOPA)
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
AUC0-∞ - Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to Infinity (L-DOPA)
|
2397 ng.h/mL
Standard Deviation 741
|
2730 ng.h/mL
Standard Deviation 913
|
2603 ng.h/mL
Standard Deviation 836
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dosePopulation: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Mean pharmacokinetic parameters of 3-O-methyl-levodopa (3-OMD)
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
Cmax - Maximum Observed Plasma Concentration (3-OMD)
|
490 ng/mL
Standard Deviation 175
|
336 ng/mL
Standard Deviation 127
|
401 ng/mL
Standard Deviation 141
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dosePopulation: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Pharmacokinetic parameters of 3-O-methyl-levodopa (3-OMD). For tmax = time to Cmax values are presented as median with range values.
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
Tmax - Time to Occurrence of Cmax (3-OMD)
|
6.00 hours
Interval 4.0 to 6.0
|
5.00 hours
Interval 4.0 to 8.0
|
5.00 hours
Interval 3.0 to 8.0
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Mean pharmacokinetic parameters of 3-O-methyl-levodopa (3-OMD)
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
AUC0-t - Area Under the Plasma Concentration-time Curve to Last Measurable Time Point (3-OMD)
|
10296 ng.h/mL
Standard Deviation 3151
|
6940 ng.h/mL
Standard Deviation 2504
|
8149 ng.h/mL
Standard Deviation 2809
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Mean pharmacokinetic parameters of 3-O-methyl-levodopa (3-OMD)
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
AUC0-∞ - Area Under the Plasma Concentration-time Curve Extrapolated to Infinity (3-OMD)
|
11193 ng.h/mL
Standard Deviation 3187
|
7730 ng.h/mL
Standard Deviation 2578
|
89962 ng.h/mL
Standard Deviation 2803
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Mean pharmacokinetic parameters of carbidopa
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
Cmax - Maximum Observed Plasma Concentration (Carbidopa)
|
134 ng/mL
Standard Deviation 56.2
|
136 ng/mL
Standard Deviation 62.0
|
142 ng/mL
Standard Deviation 71.3
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Pharmacokinetic parameters of carbidopa. For tmax = time to Cmax values are presented as median with range values.
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
Tmax - Time to Occurrence of Cmax (Carbidopa)
|
3.00 hours
Interval 1.5 to 4.0
|
3.00 hours
Interval 1.0 to 4.0
|
3.00 hours
Interval 1.0 to 4.0
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Mean pharmacokinetic parameters of carbidopa
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
AUC0-t - Area Under the Plasma Concentration-time Curve to Last Measurable Time Point (Carbidopa)
|
656 ng.h/mL
Standard Deviation 226
|
670 ng.h/mL
Standard Deviation 253
|
732 ng.h/mL
Standard Deviation 335
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dosePopulation: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Pharmacokinetic parameters of carbidopa. For tmax = time to Cmax values are presented as median with range values.
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
AUC0-∞ - Area Under the Plasma Concentration-time Curve Extrapolated to Infinity (Carbidopa)
|
668 ng.h/mL
Standard Deviation 224
|
683 ng.h/mL
Standard Deviation 253
|
745 ng.h/mL
Standard Deviation 337
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Mean pharmacokinetic parameters of BIA 9-1067
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=18 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
Cmax - Maximum Observed Plasma Concentration (BIA 9-1067)
|
648 ng/mL
Standard Deviation 264
|
625 ng/mL
Standard Deviation 346
|
628 ng/mL
Standard Deviation 295
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Pharmacokinetic parameters of BIA 9-1067. For tmax = time to Cmax values are presented as median with range values.
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=18 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
Tmax - Time to Occurrence of Cmax (BIA 9-1067)
|
2.50 hours
Interval 1.0 to 6.0
|
3.50 hours
Interval 0.5 to 6.0
|
4.00 hours
Interval 2.0 to 6.0
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Mean pharmacokinetic parameters of BIA 9-1067
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=18 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
AUC0-t - Area Under the Plasma Concentration-time Curve to Last Measurable Time Point (BIA 9-1067)
|
2094 ng.h/mL
Standard Deviation 904
|
2130 ng.h/mL
Standard Deviation 1248
|
2245 ng.h/mL
Standard Deviation 1171
|
PRIMARY outcome
Timeframe: Pre-dose, ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48 and 72 h after dose.Population: According to the protocol, the "pharmacokinetic population" should include all subjects who had valid data for all treatment periods. In this study, 18 subjects completed 2 treatment periods, 17 subjects completed 3 treatment periods and 16 subjects completed all 4 treatment periods.
Mean pharmacokinetic parameters of BIA 9-1067
Outcome measures
| Measure |
Sinemet® 100/25 mg
n=17 Participants
Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=15 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=11 Participants
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly BIA 9-1067 Levodopa 100 mg Carbidopa 25 mg
|
|---|---|---|---|
|
AUC0-∞ - Area Under the Plasma Concentration-time Curve Extrapolated to Infinity (BIA 9-1067)
|
2165 ng.h/mL
Standard Deviation 913
|
2360 ng.h/mL
Standard Deviation 1281
|
2678 ng.h/mL
Standard Deviation 1334
|
Adverse Events
BIA 9-1067 50 mg
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
Sinemet® 100/25 mg
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
BIA 9-1067 50 mg
n=18 participants at risk
BIA 9-1067 50 mg.
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Separated 1 h
n=18 participants at risk
BIA 9-1067 50 mg + Sinemet® 100/25 mg separated 1 h.
|
BIA 9-1067 50 mg + Sinemet® 100/25 mg Concomitantly
n=16 participants at risk
BIA 9-1067 50 mg + Sinemet® 100/25 mg concomitantly.
|
Sinemet® 100/25 mg
n=17 participants at risk
Sinemet® 100/25 mg.
|
|---|---|---|---|---|
|
Eye disorders
Ocular hyperaemia
|
0.00%
0/18
|
0.00%
0/18
|
0.00%
0/16
|
5.9%
1/17
|
|
Gastrointestinal disorders
Abdominal pain
|
0.00%
0/18
|
5.6%
1/18
|
0.00%
0/16
|
5.9%
1/17
|
|
Gastrointestinal disorders
Constipation
|
5.6%
1/18
|
0.00%
0/18
|
0.00%
0/16
|
0.00%
0/17
|
|
Gastrointestinal disorders
Diarrhoea
|
0.00%
0/18
|
5.6%
1/18
|
0.00%
0/16
|
0.00%
0/17
|
|
Gastrointestinal disorders
Flatulence
|
0.00%
0/18
|
0.00%
0/18
|
6.2%
1/16
|
0.00%
0/17
|
|
Gastrointestinal disorders
Gingival pain
|
0.00%
0/18
|
5.6%
1/18
|
0.00%
0/16
|
0.00%
0/17
|
|
Gastrointestinal disorders
Nausea
|
5.6%
1/18
|
5.6%
1/18
|
0.00%
0/16
|
5.9%
1/17
|
|
General disorders
Asthenia
|
0.00%
0/18
|
5.6%
1/18
|
0.00%
0/16
|
0.00%
0/17
|
|
General disorders
Fatigue
|
5.6%
1/18
|
0.00%
0/18
|
0.00%
0/16
|
5.9%
1/17
|
|
General disorders
Pyrexia
|
0.00%
0/18
|
5.6%
1/18
|
0.00%
0/16
|
0.00%
0/17
|
|
Investigations
Blood creatine phosphokinase increased
|
0.00%
0/18
|
5.6%
1/18
|
0.00%
0/16
|
0.00%
0/17
|
|
Investigations
Blood pressure systolic decreased
|
0.00%
0/18
|
0.00%
0/18
|
0.00%
0/16
|
5.9%
1/17
|
|
Investigations
Blood pressure systolic increased
|
5.6%
1/18
|
0.00%
0/18
|
0.00%
0/16
|
0.00%
0/17
|
|
Musculoskeletal and connective tissue disorders
Back pain
|
0.00%
0/18
|
0.00%
0/18
|
0.00%
0/16
|
11.8%
2/17
|
|
Nervous system disorders
Dizziness
|
5.6%
1/18
|
0.00%
0/18
|
6.2%
1/16
|
5.9%
1/17
|
|
Nervous system disorders
Dysgeusia
|
0.00%
0/18
|
0.00%
0/18
|
6.2%
1/16
|
0.00%
0/17
|
|
Nervous system disorders
Headache
|
11.1%
2/18
|
16.7%
3/18
|
25.0%
4/16
|
23.5%
4/17
|
|
Nervous system disorders
Somnolence
|
33.3%
6/18
|
22.2%
4/18
|
25.0%
4/16
|
29.4%
5/17
|
|
Respiratory, thoracic and mediastinal disorders
Cough
|
5.6%
1/18
|
0.00%
0/18
|
0.00%
0/16
|
0.00%
0/17
|
|
Respiratory, thoracic and mediastinal disorders
Dry throat
|
0.00%
0/18
|
5.6%
1/18
|
0.00%
0/16
|
0.00%
0/17
|
|
Respiratory, thoracic and mediastinal disorders
Nasal congestion
|
0.00%
0/18
|
5.6%
1/18
|
0.00%
0/16
|
0.00%
0/17
|
|
Respiratory, thoracic and mediastinal disorders
Oropharyngeal pain
|
0.00%
0/18
|
5.6%
1/18
|
12.5%
2/16
|
0.00%
0/17
|
|
Respiratory, thoracic and mediastinal disorders
Rhinorrhoea
|
0.00%
0/18
|
11.1%
2/18
|
6.2%
1/16
|
0.00%
0/17
|
|
Skin and subcutaneous tissue disorders
Acne
|
0.00%
0/18
|
0.00%
0/18
|
6.2%
1/16
|
5.9%
1/17
|
|
Skin and subcutaneous tissue disorders
Pruritus
|
5.6%
1/18
|
5.6%
1/18
|
0.00%
0/16
|
0.00%
0/17
|
|
Skin and subcutaneous tissue disorders
Rash
|
0.00%
0/18
|
11.1%
2/18
|
6.2%
1/16
|
5.9%
1/17
|
|
Skin and subcutaneous tissue disorders
Rash Pruritic
|
0.00%
0/18
|
5.6%
1/18
|
0.00%
0/16
|
0.00%
0/17
|
Additional Information
Head of Clinical Research
Bial - Portela & Cª, S.A.
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: OTHER