MedPath

Pharmacokinetic Interaction Study Between Eslicarbazepine Acetate and Carbamazepine

Phase 1
Completed
Conditions
Epilepsy
Interventions
Registration Number
NCT02284854
Lead Sponsor
Bial - Portela C S.A.
Brief Summary

Open-label study in two parallel groups of 20 healthy subjects each. Group A assessed the effect of CBZ on ESL pharmacokinetics, and Group B assessed the effect of ESL on CBZ pharmacokinetics.

Detailed Description

Open-label study in two parallel groups of 20 healthy subjects each. Group A assessed the effect of CBZ on ESL pharmacokinetics, and Group B assessed the effect of ESL on CBZ pharmacokinetics. Each patient participated in the study for approximately 9 weeks. The clinical portion of the study was completed in approximately 3 months. Subjects received the treatments during 35 days.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
43
Inclusion Criteria
  • Male and female subjects aged 18 to 45 years inclusive;
  • Body mass index (BMI) between 18 and 30 kg/m2 inclusive;
  • Healthy as determined by pre-study medical history, physical examination, vital signs, and 12-lead electrocardiogram (ECG); negative tests for Hepatitis B surface Antigen (HBsAg), anti-HCVAb and Human Immunodeficiency Virus (HIV)-1 and HIV-2 Ab at screening;
  • Clinical laboratory test results clinically acceptable at screening and admission to each treatment period;
  • Negative screen for alcohol and drugs of abuse at screening and admission to each treatment period;
  • Non-smokers or ex-smokers;
  • Able and willing to give written informed consent;
  • If female, not of childbearing potential by reason of surgery or, if of childbearing potential, she used a double-barrier method of contraception: 1 male barrier method [male condom] plus 1 female barrier method (diaphragm, spermicide, or intrauterine device);
  • If female, had a negative urine pregnancy test at screening and admission to each treatment period.
Exclusion Criteria
  • 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; have a clinically relevant surgical history;
  • History of relevant atopy or any drug hypersensitivity (including known hypersensitivity to ESL or other carboxamide derivatives [e.g., carbamazepine, oxcarbazepine] or any of its excipients; known hypersensitivity to drugs structurally related to carbamazepine [e.g.: tricyclic antidepressants] or any of its excipients);
  • Second or third-degree atrioventricular blockade not corrected with a pace-maker or any other clinically significant abnormality in the 12-lead ECG as determined by the investigator;
  • History of alcoholism or drug abuse;
  • Consumed more than 14 units1 of alcohol a week;
  • Significant infection or known inflammatory process on screening or admission to each treatment period;
  • Acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission to each treatment period;
  • Use of medicines within two weeks of admission to first period that may affect the safety or other study assessments, in the investigator's opinion;
  • Had donated or received any blood or blood products within the 3 months prior to screening;
  • Vegetarians, vegans or have other medical dietary restrictions;
  • Could not communicate reliably with the investigator; was unlikely to co-operate with the requirements of the study;
  • Unwilling or unable to give written informed consent;
  • If female, was pregnant or breast-feeding;
  • If female, was of childbearing potential and did not use an accepted effective contraceptive method or used hormonal contraceptives;
  • Had received an investigational drug within 3 months of screening or was currently participating in another study.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Group BBIA 2-093Day 1 to Day 8 - CBZ 200 mg Day 9 to Day 14 - CBZ 400 mg Day 15 to Day 29 - CBZ 400 mg twice-daily Day 30 to Day 35 - BIA 2-093 800 mg + CBZ 400 mg twice-daily
Group ABIA 2-093Day 1 to Day 8 - BIA 2-093 800 mg Day 9 to Day 14 - BIA 2-093 800 mg + CBZ 200 mg Day 15 to Day 22 - BIA 2-093 800 mg + CBZ 400 mg Day 23 to Day 35 - BIA 2-093 800 mg + CBZ 400 mg twice-daily
Group ACarbamazepineDay 1 to Day 8 - BIA 2-093 800 mg Day 9 to Day 14 - BIA 2-093 800 mg + CBZ 200 mg Day 15 to Day 22 - BIA 2-093 800 mg + CBZ 400 mg Day 23 to Day 35 - BIA 2-093 800 mg + CBZ 400 mg twice-daily
Group BCarbamazepineDay 1 to Day 8 - CBZ 200 mg Day 9 to Day 14 - CBZ 400 mg Day 15 to Day 29 - CBZ 400 mg twice-daily Day 30 to Day 35 - BIA 2-093 800 mg + CBZ 400 mg twice-daily
Primary Outcome Measures
NameTimeMethod
Cmax (CBZ) - the Maximum Plasma ConcentrationDay 28 to 35

Reference - Day 28 following twice-daily oral administration of CBZ 400 mg Test - Day 35 following twice-daily oral administration of CBZ 400 mg

AUC0-t (CBZ) - Area Under the Curve to Last Measurable Concentration for CBZDay 28 to 35

Reference - Day 28 following twice-daily oral administration of CBZ 400 mg Test - Day 35 following twice-daily oral administration of CBZ 400 mg

AUC0-t (CBZE) - Area Under the Curve to Last Measurable Concentration for CBZEDay 28 to 35

Reference - Day 28 following twice-daily oral administration of CBZ 400 mg Test - Day 35 following twice-daily oral administration of CBZ 400 mg

CBZE - carbamazepine-epoxide is the active metabolite of CBZ

Cmax (BIA 2-093) - the Maximum Plasma ConcentrationDay 7 to 35

Reference - Day 7 following once-daily oral administration of ESL 800 mg Test - Day 35 following once-daily oral administration of ESL 800 mg

Cmax (CBZE) - the Maximum Plasma ConcentrationDay 28 to 35

Reference - Day 28 following twice-daily oral administration of CBZ 400 mg twice-daily Test - Day 35 following twice-daily oral administration of CBZ 400 mg twice-daily

CBZE - carbamazepine-epoxide is the active metabolite of CBZ

AUC0-t (BIA 2-093) - Area Under the Curve to Last Measurable Concentration for BIA 2-093Day 7 to 35

Reference - Day 7 following once-daily oral administration of ESL 800 mg Test - Day 35 following once-daily oral administration of ESL 800 mg

Secondary Outcome Measures
NameTimeMethod
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