Trial Outcomes & Findings for Disposition of Eslicarbazepine Acetate and Its Metabolites S-licarbazepine and R-licarbazepine (NCT NCT02281591)
NCT ID: NCT02281591
Last Updated: 2025-04-08
Results Overview
BIA 2-194, BIA 2-195 and Oxcarbazepine are metabolites of BIA 2-093 and Licarbazepine.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
32 participants
Primary outcome timeframe
Phase A: pre-dose (Day 1); and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72 and 96 hours post-dose.Phase B: Days 6 to 10 inclusively: pre-dose. Day 11 (last dose): pre-dose; and ½, 1, 1½,2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72 and 96 hours post-dose.
Results posted on
2025-04-08
Participant Flow
Participant milestones
| Measure |
Eslicarbazepine Acetate
900mg of eslicarbazepine acetate (ESL, BIA 2-093)
BIA 2-093: Tablets containing 900 mg
|
S-licarbazepine R-licarbazepine
450 mg of S-licarbazepine plus 450 mg of R-licarbazepine
S-licarbazepine: capsules containing 225 mg
R-licarbazepine: capsules containing 225 mg
|
S-licarbazepine
450 mg of S-licarbazepine
S-licarbazepine: capsules containing 225 mg
|
R-licarbazepine
450 mg of Rlicarbazepine
R-licarbazepine: capsules containing 225 mg
|
|---|---|---|---|---|
|
Overall Study
STARTED
|
8
|
8
|
8
|
8
|
|
Overall Study
COMPLETED
|
8
|
8
|
8
|
8
|
|
Overall Study
NOT COMPLETED
|
0
|
0
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
Disposition of Eslicarbazepine Acetate and Its Metabolites S-licarbazepine and R-licarbazepine
Baseline characteristics by cohort
| Measure |
Eslicarbazepine Acetate
n=8 Participants
900mg of eslicarbazepine acetate (ESL, BIA 2-093)
BIA 2-093: Tablets containing 900 mg
|
S-licarbazepine R-licarbazepine
n=8 Participants
450 mg of S-licarbazepine plus 450 mg of R-licarbazepine
S-licarbazepine: capsules containing 225 mg
R-licarbazepine: capsules containing 225 mg
|
S-licarbazepine
n=8 Participants
450 mg of S-licarbazepine
S-licarbazepine: capsules containing 225 mg
|
R-licarbazepine
n=8 Participants
450 mg of Rlicarbazepine
R-licarbazepine: capsules containing 225 mg
|
Total
n=32 Participants
Total of all reporting groups
|
|---|---|---|---|---|---|
|
Age, Categorical
<=18 years
|
0 Participants
n=93 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=27 Participants
|
0 Participants
n=483 Participants
|
0 Participants
n=36 Participants
|
|
Age, Categorical
Between 18 and 65 years
|
8 Participants
n=93 Participants
|
8 Participants
n=4 Participants
|
8 Participants
n=27 Participants
|
8 Participants
n=483 Participants
|
32 Participants
n=36 Participants
|
|
Age, Categorical
>=65 years
|
0 Participants
n=93 Participants
|
0 Participants
n=4 Participants
|
0 Participants
n=27 Participants
|
0 Participants
n=483 Participants
|
0 Participants
n=36 Participants
|
|
Sex: Female, Male
Female
|
4 Participants
n=93 Participants
|
4 Participants
n=4 Participants
|
4 Participants
n=27 Participants
|
4 Participants
n=483 Participants
|
16 Participants
n=36 Participants
|
|
Sex: Female, Male
Male
|
4 Participants
n=93 Participants
|
4 Participants
n=4 Participants
|
4 Participants
n=27 Participants
|
4 Participants
n=483 Participants
|
16 Participants
n=36 Participants
|
PRIMARY outcome
Timeframe: Phase A: pre-dose (Day 1); and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72 and 96 hours post-dose.Phase B: Days 6 to 10 inclusively: pre-dose. Day 11 (last dose): pre-dose; and ½, 1, 1½,2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72 and 96 hours post-dose.BIA 2-194, BIA 2-195 and Oxcarbazepine are metabolites of BIA 2-093 and Licarbazepine.
Outcome measures
| Measure |
Eslicarbazepine Acetate
n=8 Participants
900mg of eslicarbazepine acetate (ESL, BIA 2-093)
BIA 2-093: Tablets containing 900 mg
|
S-licarbazepine R-licarbazepine
n=8 Participants
450 mg of S-licarbazepine plus 450 mg of R-licarbazepine
S-licarbazepine: capsules containing 225 mg
R-licarbazepine: capsules containing 225 mg
|
S-licarbazepine
n=8 Participants
450 mg of S-licarbazepine
S-licarbazepine: capsules containing 225 mg
|
R-licarbazepine
n=8 Participants
450 mg of Rlicarbazepine
R-licarbazepine: capsules containing 225 mg
|
|---|---|---|---|---|
|
Cmax - the Maximum Plasma Concentration
Cmax (BIA 2-194)
|
15809 ng/mL
Standard Deviation 3183
|
10496 ng/mL
Standard Deviation 1432
|
10364 ng/mL
Standard Deviation 3352
|
437 ng/mL
Standard Deviation 143
|
|
Cmax - the Maximum Plasma Concentration
Cmax (BIA 2-195)
|
222 ng/mL
Standard Deviation 68.4
|
8099 ng/mL
Standard Deviation 1258
|
132 ng/mL
Standard Deviation 29.6
|
6941 ng/mL
Standard Deviation 1054
|
|
Cmax - the Maximum Plasma Concentration
Cmax (Oxcarbazepine)
|
136 ng/mL
Standard Deviation 25.1
|
261 ng/mL
Standard Deviation 53.5
|
92.8 ng/mL
Standard Deviation 21.8
|
101 ng/mL
Standard Deviation 28.6
|
PRIMARY outcome
Timeframe: Phase A: pre-dose (Day 1); and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72 and 96 hours post-dose.Phase B: Days 6 to 10 inclusively: pre-dose. Day 11 (last dose): pre-dose; and ½, 1, 1½,2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72 and 96 hours post-dose.BIA 2-194, BIA 2-195 and Oxcarbazepine are metabolites of BIA 2-093 and Licarbazepine.
Outcome measures
| Measure |
Eslicarbazepine Acetate
n=8 Participants
900mg of eslicarbazepine acetate (ESL, BIA 2-093)
BIA 2-093: Tablets containing 900 mg
|
S-licarbazepine R-licarbazepine
n=8 Participants
450 mg of S-licarbazepine plus 450 mg of R-licarbazepine
S-licarbazepine: capsules containing 225 mg
R-licarbazepine: capsules containing 225 mg
|
S-licarbazepine
n=8 Participants
450 mg of S-licarbazepine
S-licarbazepine: capsules containing 225 mg
|
R-licarbazepine
n=8 Participants
450 mg of Rlicarbazepine
R-licarbazepine: capsules containing 225 mg
|
|---|---|---|---|---|
|
Tmax - the Time of Occurrence of Cmax
tmax (BIA 2-194)
|
1.99 hours
Standard Deviation 0.916
|
1.01 hours
Standard Deviation 0.320
|
0.965 hours
Standard Deviation 0.496
|
10.7 hours
Standard Deviation 3.69
|
|
Tmax - the Time of Occurrence of Cmax
tmax (BIA 2-195)
|
18.6 hours
Standard Deviation 4.14
|
1.41 hours
Standard Deviation 0.320
|
11.7 hours
Standard Deviation 3.77
|
1.22 hours
Standard Deviation 0.582
|
|
Tmax - the Time of Occurrence of Cmax
tmax (Oxcarbazepine)
|
3.59 hours
Standard Deviation 1.61
|
1.34 hours
Standard Deviation 0.354
|
1.36 hours
Standard Deviation 1.44
|
1.21 hours
Standard Deviation 0.641
|
PRIMARY outcome
Timeframe: Phase A: pre-dose (Day 1); and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72 and 96 hours post-dose.Phase B: Days 6 to 10 inclusively: pre-dose. Day 11 (last dose): pre-dose; and ½, 1, 1½,2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72 and 96 hours post-dose.BIA 2-194, BIA 2-195 and Oxcarbazepine are metabolites of BIA 2-093 and Licarbazepine.
Outcome measures
| Measure |
Eslicarbazepine Acetate
n=8 Participants
900mg of eslicarbazepine acetate (ESL, BIA 2-093)
BIA 2-093: Tablets containing 900 mg
|
S-licarbazepine R-licarbazepine
n=8 Participants
450 mg of S-licarbazepine plus 450 mg of R-licarbazepine
S-licarbazepine: capsules containing 225 mg
R-licarbazepine: capsules containing 225 mg
|
S-licarbazepine
n=8 Participants
450 mg of S-licarbazepine
S-licarbazepine: capsules containing 225 mg
|
R-licarbazepine
n=8 Participants
450 mg of Rlicarbazepine
R-licarbazepine: capsules containing 225 mg
|
|---|---|---|---|---|
|
AUC0-∞ - the Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity
AUC0-∞ (BIA 2-194)
|
271191 ng.h/mL
Standard Deviation 47416
|
201409 ng.h/mL
Standard Deviation 37377
|
132724 ng.h/mL
Standard Deviation 20175
|
11003 ng.h/mL
Standard Deviation 4476
|
|
AUC0-∞ - the Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity
AUC0-∞ (BIA 2-195)
|
8816 ng.h/mL
Standard Deviation 2168
|
116884 ng.h/mL
Standard Deviation 22425
|
5417 ng.h/mL
Standard Deviation 824
|
66087 ng.h/mL
Standard Deviation 16072
|
|
AUC0-∞ - the Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity
AUC0-∞ (Oxcarbazepine)
|
3181 ng.h/mL
Standard Deviation 1078
|
4726 ng.h/mL
Standard Deviation 1163
|
2500 ng.h/mL
Standard Deviation 1923
|
1073 ng.h/mL
Standard Deviation 793
|
SECONDARY outcome
Timeframe: Phase A: pre-dose (Day 1); and ½, 1, 1½, 2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72 and 96 hours post-dose.Phase B: Days 6 to 10 inclusively: pre-dose. Day 11 (last dose): pre-dose; and ½, 1, 1½,2, 3, 4, 6, 8, 12, 16, 24, 36, 48, 72 and 96 hours post-dose.BIA 2-194, BIA 2-195 and Oxcarbazepine are metabolites of BIA 2-093 and Licarbazepine.
Outcome measures
| Measure |
Eslicarbazepine Acetate
n=8 Participants
900mg of eslicarbazepine acetate (ESL, BIA 2-093)
BIA 2-093: Tablets containing 900 mg
|
S-licarbazepine R-licarbazepine
n=8 Participants
450 mg of S-licarbazepine plus 450 mg of R-licarbazepine
S-licarbazepine: capsules containing 225 mg
R-licarbazepine: capsules containing 225 mg
|
S-licarbazepine
n=8 Participants
450 mg of S-licarbazepine
S-licarbazepine: capsules containing 225 mg
|
R-licarbazepine
n=8 Participants
450 mg of Rlicarbazepine
R-licarbazepine: capsules containing 225 mg
|
|---|---|---|---|---|
|
AUC0-t - the Area Under the Plasma Concentration-time Curve to Last Measurable Time Point
AUC0-t (BIA 2-194)
|
268045 ng.h/mL
Standard Deviation 46861
|
198313 ng.h/mL
Standard Deviation 38771
|
130147 ng.h/mL
Standard Deviation 19326
|
9419 ng.h/mL
Standard Deviation 4707
|
|
AUC0-t - the Area Under the Plasma Concentration-time Curve to Last Measurable Time Point
AUC0-t (BIA 2-195)
|
6757 ng.h/mL
Standard Deviation 2211
|
114635 ng.h/mL
Standard Deviation 21741
|
3074 ng.h/mL
Standard Deviation 1001
|
65203 ng.h/mL
Standard Deviation 16161
|
|
AUC0-t - the Area Under the Plasma Concentration-time Curve to Last Measurable Time Point
AUC0-t (Oxcarbazepine)
|
1947 ng.h/mL
Standard Deviation 757
|
3401 ng.h/mL
Standard Deviation 902
|
748 ng.h/mL
Standard Deviation 308
|
422 ng.h/mL
Standard Deviation 247
|
Adverse Events
Eslicarbazepine Acetate
Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths
S-licarbazepine R-licarbazepine
Serious events: 0 serious events
Other events: 8 other events
Deaths: 0 deaths
S-licarbazepine
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
R-licarbazepine
Serious events: 0 serious events
Other events: 5 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Eslicarbazepine Acetate
n=8 participants at risk
900mg of eslicarbazepine acetate (ESL, BIA 2-093)
BIA 2-093: Tablets containing 900 mg
|
S-licarbazepine R-licarbazepine
n=8 participants at risk
450 mg of S-licarbazepine plus 450 mg of R-licarbazepine
S-licarbazepine: capsules containing 225 mg
R-licarbazepine: capsules containing 225 mg
|
S-licarbazepine
n=8 participants at risk
450 mg of S-licarbazepine
S-licarbazepine: capsules containing 225 mg
|
R-licarbazepine
n=8 participants at risk
450 mg of Rlicarbazepine
R-licarbazepine: capsules containing 225 mg
|
|---|---|---|---|---|
|
Eye disorders
Burning sensation in eye
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Eye disorders
Visual disturbance
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
12.5%
1/8
|
|
Gastrointestinal disorders
Dry mouth
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Gastrointestinal disorders
Nausea
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Gastrointestinal disorders
Numbness of tongue
|
0.00%
0/8
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Gastrointestinal disorders
Oral dryness
|
0.00%
0/8
|
12.5%
1/8
|
0.00%
0/8
|
12.5%
1/8
|
|
Gastrointestinal disorders
Paraesthesia lips
|
0.00%
0/8
|
25.0%
2/8
|
12.5%
1/8
|
0.00%
0/8
|
|
Gastrointestinal disorders
Paraesthesia tongue
|
0.00%
0/8
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Gastrointestinal disorders
Vomiting
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
|
General disorders
Feeling hungry
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
|
General disorders
Tiredness
|
12.5%
1/8
|
75.0%
6/8
|
12.5%
1/8
|
25.0%
2/8
|
|
Infections and infestations
Vaginal infection
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
12.5%
1/8
|
|
Injury, poisoning and procedural complications
Accidental injury
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Musculoskeletal and connective tissue disorders
Leg pain
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
12.5%
1/8
|
|
Nervous system disorders
Acroparaesthesia
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Nervous system disorders
Concentration loss
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Nervous system disorders
Dizziness
|
25.0%
2/8
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Nervous system disorders
Head pressure
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
12.5%
1/8
|
|
Nervous system disorders
Headache
|
37.5%
3/8
|
37.5%
3/8
|
12.5%
1/8
|
12.5%
1/8
|
|
Psychiatric disorders
Increased libido
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
12.5%
1/8
|
|
Skin and subcutaneous tissue disorders
Blister of fingers, without mention of infection
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Skin and subcutaneous tissue disorders
Herpes labialis
|
0.00%
0/8
|
0.00%
0/8
|
12.5%
1/8
|
0.00%
0/8
|
|
Skin and subcutaneous tissue disorders
Itching
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Skin and subcutaneous tissue disorders
Bulla dorsum manus
|
0.00%
0/8
|
12.5%
1/8
|
0.00%
0/8
|
0.00%
0/8
|
|
Surgical and medical procedures
Tooth extraction
|
0.00%
0/8
|
0.00%
0/8
|
12.5%
1/8
|
0.00%
0/8
|
Additional Information
Head of Clinical Research
Bial - Portela & Cª, S.A.
Phone: +351 229 866 100
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: OTHER