Disposition of Eslicarbazepine Acetate and Its Metabolites S-licarbazepine and R-licarbazepine

Phase 1

Completed

• Conditions: Epilepsy
• Interventions: Drug: BIA 2-093; Drug: S-licarbazepine; Drug: R-licarbazepine

• Registration Number: NCT02281591
• Lead Sponsor: Bial - Portela C S.A.

Brief Summary

Single centre, open-label, randomised study in four parallel groups of healthy volunteers

Detailed Description

Single centre, open-label, randomised study in four parallel groups of healthy volunteers: Group 1 = 900 mg of eslicarbazepine acetate (ESL, BIA 2-093); Group 2 = 450 mg of S-licarbazepine plus 450 mg of R-licarbazepine; Group 3 = 450 mg of S-licarbazepine; Group 4 = 450 mg of Rlicarbazepine. In each group, the study consisted of a single-dose period (Phase A) followed by a repeateddose period of 7 days of duration in which the investigational product was administered once daily (Phase B). The repeated-dose phase started 96 h post single-dose.

Study Timeline

• Study Start: 2006-06
• Primary Completion: 2006-07
• Study Completion: 2006-07
• Study First Submitted: 2014-10-30
• Study First Submitted QC: 2014-10-30
• Study First Posted: 2014-11-02
• Results First Submitted: 2014-11-28
• Results First Submitted QC: 2014-11-28
• Results First Posted: 2014-12-03
• Status Verified: 2025-03
• Last Update Submitted: 2025-03-25
• Last Update Posted: 2025-04-08

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 32

Inclusion Criteria

Not provided

Exclusion Criteria

• Subjects who did not conform to the above inclusion criteria, OR
• Subjects who had a clinically relevant history or presence of respiratory, gastrointestinal, renal, hepatic, haematological, lymphatic, neurological, cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological, dermatological, endocrine, connective tissue diseases or disorders.
• Subjects who had a clinically relevant surgical history.
• Subjects who had a clinically relevant family history.
• Subjects who had a history of relevant atopy.
• Subjects who had a history of relevant drug hypersensitivity (especially carbamazepine or oxcarbazepine).
• Subjects who had a history of alcoholism or drug abuse.
• Subjects who consumed more than 14 units of alcohol a week.
• Subjects who had a significant infection or known inflammatory process on screening or admission.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
eslicarbazepine acetate	BIA 2-093	900mg of eslicarbazepine acetate (ESL, BIA 2-093)
S-licarbazepine R-licarbazepine	S-licarbazepine	450 mg of S-licarbazepine plus 450 mg of R-licarbazepine
R-licarbazepine	R-licarbazepine	450 mg of Rlicarbazepine
S-licarbazepine R-licarbazepine	R-licarbazepine	450 mg of S-licarbazepine plus 450 mg of R-licarbazepine
S-licarbazepine	S-licarbazepine	450 mg of S-licarbazepine

Primary Outcome Measures

Name	Time	Method
Cmax - the Maximum Plasma Concentration	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.
Tmax - the Time of Occurrence of Cmax	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.
AUC0-∞ - the Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity	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.

Secondary Outcome Measures

Name	Time	Method
AUC0-t - the Area Under the Plasma Concentration-time Curve to Last Measurable Time Point	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.

Trial Locations

Locations (1)

Scope International Life Sciences AG,; 🇩🇪 Hamburg, Germany