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

BIAL

Status and phase: Completed; Phase 1

Conditions: Epilepsy

Treatments: Drug: S-licarbazepine; Drug: BIA 2-093; Drug: R-licarbazepine

Study type: Interventional

Funder types: Industry

Identifiers

NCT02281591

BIA-2093-115

Details and patient eligibility

About

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

Full 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.

Enrollment: 32 patients

Sex: All

Ages: 18 to 45 years old

Volunteers: Accepts Healthy Volunteers

Inclusion and exclusion 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.

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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32 participants in 4 patient groups

eslicarbazepine acetate

Experimental group

Description:

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

Treatment:

Drug: BIA 2-093

S-licarbazepine R-licarbazepine

Active Comparator group

Description:

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

Treatment:

Drug: R-licarbazepine

Drug: S-licarbazepine

S-licarbazepine

Active Comparator group

Description:

450 mg of S-licarbazepine

Treatment:

Drug: S-licarbazepine

R-licarbazepine

Active Comparator group

Description:

450 mg of Rlicarbazepine

Treatment:

Drug: R-licarbazepine