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

NCT02281591 | Completed Phase 1 Results

• 1 other identifier: BIA-2093-115
• Study Type: interventional
• Target: 32
• Locations: 1 country
• Sites: 1

Brief Summary

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

Conditions

Epilepsy

Outcome Measures

Primary Outcomes (3)

• Cmax - the Maximum Plasma Concentration

  BIA 2-194, BIA 2-195 and Oxcarbazepine are metabolites of BIA 2-093 and Licarbazepine.

  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.

• Tmax - the Time of Occurrence of Cmax

  BIA 2-194, BIA 2-195 and Oxcarbazepine are metabolites of BIA 2-093 and Licarbazepine.

  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.

• AUC0-∞ - the Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity

  BIA 2-194, BIA 2-195 and Oxcarbazepine are metabolites of BIA 2-093 and Licarbazepine.

  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.

Secondary Outcomes (1)

• 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.

Study Arms (4)

eslicarbazepine acetate

EXPERIMENTAL

900mg of eslicarbazepine acetate (ESL, BIA 2-093)

Drug: BIA 2-093

S-licarbazepine R-licarbazepine

ACTIVE COMPARATOR

450 mg of S-licarbazepine plus 450 mg of R-licarbazepine

Drug: S-licarbazepine; Drug: R-licarbazepine

S-licarbazepine

ACTIVE COMPARATOR

450 mg of S-licarbazepine

Drug: S-licarbazepine

R-licarbazepine

ACTIVE COMPARATOR

450 mg of Rlicarbazepine

Drug: R-licarbazepine

Interventions

BIA 2-093 DRUG

Tablets containing 900 mg

eslicarbazepine acetate

S-licarbazepine DRUG

capsules containing 225 mg

S-licarbazepine; S-licarbazepine R-licarbazepine

R-licarbazepine DRUG

capsules containing 225 mg

R-licarbazepine; S-licarbazepine R-licarbazepine

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Male or female subjects aged between 18 and 45 years, inclusive.
• Subjects of body mass index (BMI) between 19 and 30 kg/m2, inclusive.
• Subjects who were healthy as determined by pre-study medical history, physical examination, vital signs, neurological examination, and 12-lead ECG.
• Subjects who had clinical laboratory tests clinically acceptable at screening and admission.
• Subjects who had negative tests for HBsAg, anti-HCV Ab and HIV-1 and HIV-2 Ab at screening.
• Subjects who were negative for drugs of abuse and alcohol at screening and admission.
• Subjects who were non-smokers or who smoke \< 10 cigarettes or equivalent per day.
• Subjects who are able and willing to give written informed consent.
• (If female) She was not of childbearing potential by reason of surgery or, if of childbearing potential, she used one of the following methods of contraception: double barrier, intrauterine device or abstinence.
• (If female) She had a negative pregnancy test at screening and admission to Phase A.

You may not qualify if:

• 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.

Sponsors & Collaborators

• Bial - Portela C S.A.: lead

Study Sites (1)

Scope International Life Sciences AG,

Hamburg, D-22525, Germany

Location

MeSH Terms

Conditions

Epilepsy

Interventions

eslicarbazepine acetate

Condition Hierarchy (Ancestors)

Brain Diseases; Central Nervous System Diseases; Nervous System Diseases

Results Point of Contact

• Title: Head of Clinical Research
• Organization: Bial - Portela & Cª, S.A.

jose.rocha@bial.com

+351 229 866 100

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: October 30, 2014
• First Posted: November 3, 2014
• Study Start: June 1, 2006
• Primary Completion: July 1, 2006
• Study Completion: July 1, 2006
• Last Updated: April 8, 2025
• Results First Posted: December 3, 2014

Record last verified: 2025-03

Locations

DE (1)