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

• ClinicalTrials.gov Identifier: NCT02281591
• Recruitment Status: Completed
• First Posted: November 2, 2014
• Results First Posted: December 3, 2014
• Last Update Posted: December 3, 2014
• Sponsor: Bial - Portela C S.A.
• Information provided by (Responsible Party): Bial - Portela C S.A.

Study Description

Brief Summary:

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

Condition or disease	Intervention/treatment	Phase
Epilepsy	Drug: BIA 2-093; Drug: S-licarbazepine; Drug: R-licarbazepine	Phase 1

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 Design

• Study Type: Interventional (Clinical Trial)
• Actual Enrollment: 32 participants
• Allocation: Randomized
• Intervention Model: Parallel Assignment
• Masking: None (Open Label)
• Primary Purpose: Treatment
• Official Title: Disposition of Eslicarbazepine Acetate and Its Metabolites S-licarbazepine and R-licarbazepine Following Oral Administration in Healthy Volunteers
• Study Start Date: June 2006
• Actual Primary Completion Date: July 2006
• Actual Study Completion Date: July 2006

Arms and Interventions

Arm	Intervention/treatment
Experimental: eslicarbazepine acetate; 900mg of eslicarbazepine acetate (ESL, BIA 2-093)	Drug: BIA 2-093; Tablets containing 900 mg
Active Comparator: S-licarbazepine R-licarbazepine; 450 mg of S-licarbazepine plus 450 mg of R-licarbazepine	Drug: S-licarbazepine; capsules containing 225 mg; Drug: R-licarbazepine; capsules containing 225 mg
Active Comparator: S-licarbazepine; 450 mg of S-licarbazepine	Drug: S-licarbazepine; capsules containing 225 mg
Active Comparator: R-licarbazepine; 450 mg of Rlicarbazepine	Drug: R-licarbazepine; capsules containing 225 mg

Outcome Measures

Primary Outcome Measures :

1. Cmax - the Maximum Plasma Concentration [ Time Frame: 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. ]
2. Tmax - the Time of Occurrence of Cmax [ Time Frame: 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. ]
3. AUC0-∞ - the Area Under the Plasma Concentration Versus Time Curve From Time Zero to Infinity [ Time Frame: 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 Outcome Measures :

1. AUC0-t - the Area Under the Plasma Concentration-time Curve to Last Measurable Time Point [ Time Frame: 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. ]

Eligibility Criteria

• Ages Eligible for Study: 18 Years to 45 Years (Adult)
• Sexes Eligible for Study: All
• Accepts Healthy Volunteers: Yes

Criteria

Inclusion Criteria

• 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.

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.

Contacts and Locations

Locations

Germany

Scope International Life Sciences AG,

Hamburg, Germany, D-22525

Sponsors and Collaborators

Bial - Portela C S.A.

More Information

• Responsible Party: Bial - Portela C S.A.
• ClinicalTrials.gov Identifier: NCT02281591
• Other Study ID Numbers: BIA-2093-115
• First Posted: November 2, 2014
• Results First Posted: December 3, 2014
• Last Update Posted: December 3, 2014
• Last Verified: November 2014

Additional relevant MeSH terms:

Epilepsy; Brain Diseases; Central Nervous System Diseases; Nervous System Diseases; Eslicarbazepine acetate; Anticonvulsants; Voltage-Gated Sodium Channel Blockers; Sodium Channel Blockers; Membrane Transport Modulators; Molecular Mechanisms of Pharmacological Action