A Study to Evaluate the Tolerability and Pharmacokinetics of Two Single and Multiple High Dose Regimens of BIA 2-093 In Healthy Volunteers

A Double-blind, Randomized, Placebo-Controlled Study to Evaluate the Tolerability and Pharmacokinetics of Two Single and Multiple High Dose Regimens of BIA 2-093 in Healthy Volunteers

Single centre, double-blind, randomised, placebo-controlled study of two dosage regimens of BIA 2-093 - 1800 mg (Group 1) and 2400 mg (Group 2) - in two groups of healthy male volunteers

Study Overview

• Status: Completed
• Conditions: Epilepsy
• Intervention / Treatment: Drug: Placebo; Drug: BIA 2-093 - 1800 mg (Group 1); Drug: BIA 2-093 - 2400 mg (Group 2)

Detailed Description

Within each group (n=9) 3 volunteers were randomised to receive placebo and the remaining 6 volunteers to receive BIA 2-093. No volunteer was a member of more than one treatment group. In each group, the study consisted of a single-dose period (Phase A) followed by a 7-day multiple-dose period (Phase B). The multiple-dose phase started 96 h post single-dose. Progression to the 2400 mg dose (Group 2) only occurred if the 1800 mg dose (Group 1) was considered to be safe and well tolerated. An appropriate interval separated the investigation of the two groups in order to permit a timely review and evaluation of safety data.

Treatment consisted of a single-dose (Phase A) followed by a once-daily dose for 7 days (Phase B). Doses were prepared as follows: Group 1 = 3 tablets of BIA 2-093 600 mg plus 1 placebo tablet, or 4 placebo tablets; Group 2 = 4 tablets of BIA 2-093 600 mg, or 4 placebo tablets.

• Study Type: Interventional
• Enrollment (Actual): 18
• Phase: Phase 1

Contacts and Locations

Study Locations

• Portugal
  • Coronado (S.Romão E S. Mamede)
    • Trofa, Coronado (S.Romão E S. Mamede), Portugal, 4745-457
      • Human Pharmacology Unit - BIAL - Portela & Ca, S.A.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 14 years to 41 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Male 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 within normal ranges 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 smoked less than 10 cigarettes or equivalent per day.
• Subjects who were able and willing to give written informed consent.

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.
• 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.
• Subjects who had acute gastrointestinal symptoms at the time of screening or admission (e.g., nausea, vomiting, diarrhoea, heartburn).
• Subjects who had used prescription or over-the-counter medication within 2 weeks of admission.
• Subjects who had used any investigational drug or participated in any clinical trial within 3 months of admission.
• Subjects who had previously received BIA 2-093.
• Subjects who had donated or received any blood or blood products within the previous 3 months prior to screening.
• Subjects who were vegetarians, vegans or had medical dietary restrictions.
• Subjects who could not communicate reliably with the investigator.
• Subjects who were unlikely to co-operate with the requirements of the study.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: Quadruple

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: BIA 2-093 - 1800 mg (Group 1); 3 tablets of BIA 2-093 600 mg	Drug: BIA 2-093 - 1800 mg (Group 1); 3 tablets of BIA 2-093; Other Names: Eslicarbazepine acetate
Experimental: BIA 2-093 - 2400 mg (Group 2); 4 tablets of BIA 2-093 600 mg	Drug: BIA 2-093 - 2400 mg (Group 2); 4 tablets of BIA 2-093 600 mg; Other Names: Eslicarbazepine acetate
Placebo Comparator: Placebo; placebo tablets	Drug: Placebo; placebo tablets; Other Names: sugar pills

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of Adverse Events Reported	investigate the tolerability of two single- and multiple-dose regimens of BIA 2-093 (1800 mg and 2400 mg)considering the Number of adverse events reported by patient	3 weeks

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax - Maximum Observed Plasma Drug Concentration	Single dose: pharmacokinetic parameters following an oral single-dose of BIA 2-093 Multiple dose: pharmacokinetic parameters following the last dose of an oral 7- day once-daily regimen of BIA 2-093 Oxcarbazepine is a BIA 2-093 metabolite	Day 1 and Day 7
Tmax - the Time of Occurrence of Cmax	Single dose: pharmacokinetic parameters following an oral single-dose of BIA 2-093 Multiple dose: pharmacokinetic parameters following the last dose of an oral 7- day once-daily regimen of BIA 2-093 Oxcarbazepine is a BIA 2-093 metabolite	Day 1 and Day 7
AUC0-τ	Single dose: pharmacokinetic parameters following an oral single-dose of BIA 2-093 Multiple dose: pharmacokinetic parameters following the last dose of an oral 7- day once-daily regimen of BIA 2-093 Oxcarbazepine is a BIA 2-093 metabolite	Day 1 and Day 7

Collaborators and Investigators

• Sponsor: Bial - Portela C S.A.
• Investigators: Principal Investigator: Manuel Vaz da Silva, MD, PhD, Human Pharmacology Unit / BIAL - Portela & Ca, S.A.

Study record dates

Study Major Dates

• Study Start: October 1, 2004
• Primary Completion (Actual): December 1, 2004
• Study Completion (Actual): December 1, 2004

Study Registration Dates

• First Submitted: June 13, 2013
• First Submitted That Met QC Criteria: June 14, 2013
• First Posted (Estimated): June 17, 2013

Study Record Updates

• Last Update Posted (Actual): April 8, 2025
• Last Update Submitted That Met QC Criteria: March 25, 2025
• Last Verified: March 1, 2025

More Information

Terms related to this study

• Keywords: Anticonvulsant
• Additional Relevant MeSH Terms: Brain Diseases; Central Nervous System Diseases; Nervous System Diseases; Epilepsy; Molecular Mechanisms of Pharmacological Action; Voltage-Gated Sodium Channel Blockers; Sodium Channel Blockers; Membrane Transport Modulators; Anticonvulsants; Eslicarbazepine acetate
• Other Study ID Numbers: BIA-2093-113