Study to Investigate the Tolerability, Steady-state Pharmacokinetics and Erythrocyte COMT Inhibition of BIA 3-202

NCT02772627 | Completed Phase 1

• 1 other identifier: BIA-3202-105
• Study Type: interventional
• Target: 22
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to investigate the tolerability and safety of three multiple dose regimens of nebicapone (BIA 3-202 100 mg, 200 mg, and 300 mg 6 times daily) in healthy volunteers. To characterise the steady-state pharmacokinetic and erythrocyte COMT inhibition profiles of nebicapone in healthy volunteers.

Conditions

Parkinson's Disease

Keywords

Parkinson's disease, Nebicapone

Outcome Measures

Primary Outcomes (8)

• Maximum observed plasma concentration (Cmax) - Nebicapone

  Mean nebicapone plasma concentration-time profiles following the last dose (Day 8) of a multiple-dose oral administration of nebicapone (100 mg, 200 mg or 300 mg, at 4-h intervals)

  Day 8

• Time of maximum observed concentration (tmax) - Nebicapone

  Mean nebicapone plasma concentration-time profiles following the last dose (Day 8) of a multiple-dose oral administration of nebicapone (100 mg, 200 mg or 300 mg, at 4-h intervals)

  Day 8

• Area under the plasma concentration time curve extrapolated to infinity (AUC0-∞) - Nebicapone

  Mean nebicapone plasma concentration-time profiles following the last dose (Day 8) of a multiple-dose oral administration of nebicapone (100 mg, 200 mg or 300 mg, at 4-h intervals)

  Day 8

• Apparent terminal elimination half-life (t1/2) - Nebicapone

  Mean nebicapone plasma concentration-time profiles following the last dose (Day 8) of a multiple-dose oral administration of nebicapone (100 mg, 200 mg or 300 mg, at 4-h intervals)

  Day 8

• Maximum observed plasma concentration (Cmax) - 3-O-methylnebicapone (BIA 3-270)

  Mean 3-O-methylnebicapone (BIA 3-270) plasma concentration-time profiles following the last dose (Day 8) of a multiple-dose oral administration of nebicapone (100 mg, 200 mg or 300 mg, at 4-h intervals)

  Day 8

• Time of maximum observed concentration (tmax) - 3-O-methylnebicapone (BIA 3-270)

  Mean 3-O-methylnebicapone (BIA 3-270) plasma concentration-time profiles following the last dose (Day 8) of a multiple-dose oral administration of nebicapone (100 mg, 200 mg or 300 mg, at 4-h intervals)

  Day 8

• Area under the plasma concentration time curve extrapolated to infinity (AUC0-∞) - 3-O-methylnebicapone (BIA 3-270)

  Mean 3-O-methylnebicapone (BIA 3-270) plasma concentration-time profiles following the last dose (Day 8) of a multiple-dose oral administration of nebicapone (100 mg, 200 mg or 300 mg, at 4-h intervals)

  Day 8

• Apparent terminal elimination half-life (t1/2) - 3-O-methylnebicapone (BIA 3-270)

  Mean 3-O-methylnebicapone (BIA 3-270) plasma concentration-time profiles following the last dose (Day 8) of a multiple-dose oral administration of nebicapone (100 mg, 200 mg or 300 mg, at 4-h intervals)

  Day 8

Study Arms (3)

Nebicapone 100 mg / Placebo

EXPERIMENTAL

Treatment consisted of nebicapone/placebo repeated administration: one dose at 4-h intervals, for 7 full days: first dose at approximately 08 h (±1 h) on Day 1 and final dose at approximately 08 h (±1 h) on Day 8. Within each group (n=8), 2 volunteers were be randomised to receive placebo and the remaining 6 volunteers to receive nebicapone.

Drug: Nebicapone; Drug: Placebo

Nebicapone 200 mg / Placebo

EXPERIMENTAL

Treatment consisted of nebicapone/placebo repeated administration: one dose at 4-h intervals, for 7 full days: first dose at approximately 08 h (±1 h) on Day 1 and final dose at approximately 08 h (±1 h) on Day 8. Within each group (n=8), 2 volunteers were be randomised to receive placebo and the remaining 6 volunteers to receive nebicapone.

Drug: Nebicapone; Drug: Placebo

Nebicapone 300 mg / Placebo

EXPERIMENTAL

Treatment consisted of nebicapone/placebo repeated administration: one dose at 4-h intervals, for 7 full days: first dose at approximately 08 h (±1 h) on Day 1 and final dose at approximately 08 h (±1 h) on Day 8. Within each group (n=8), 2 volunteers were be randomised to receive placebo and the remaining 6 volunteers to receive nebicapone.

Drug: Nebicapone; Drug: Placebo

Interventions

Nebicapone DRUG

Nebicapone 100 mg tablets; oral route.

Also known as: BIA 3-202

Nebicapone 100 mg / Placebo; Nebicapone 200 mg / Placebo; Nebicapone 300 mg / Placebo

Placebo DRUG

Placebo tablets; oral route.

Nebicapone 100 mg / Placebo; Nebicapone 200 mg / Placebo; Nebicapone 300 mg / Placebo

Eligibility Criteria

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

You may qualify if:

• Male and female subjects aged between 18 and 45 years, inclusive.
• Subjects of body mass index (BMI) between 19 and 28 kg/m2, inclusive.
• Subjects who were healthy as determined by pre study medical history, physical examination, and 12- lead ECG.
• Subjects who had clinical laboratory tests acceptable to the investigator.
• Subjects who were negative for HBsAg, anti-HCV Ab and HIV-1 and HIV-2 Ab tests at screening.
• Subjects who were negative for drugs of abuse and alcohol at screening and admission.
• Subjects who were non-smokers or who smoke less than 10 cigarettes or equivalent per day.
• Subjects who were 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.

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, 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 21 units of alcohol a week.
• Subjects who had a significant infection or known inflammatory process on screening and/or admission.
• Subjects who had acute gastrointestinal symptoms at the time of screening and/or admission (e.g., nausea, vomiting, diarrhoea, heartburn).
• Subjects who had an acute infection such as influenza at the time of screening and/or admission.
• Subjects who had used prescription drugs within 4 weeks of first dosing.
• Subjects who had used oral contraceptives or over the counter medication excluding oral routine vitamins but including mega dose vitamin therapy within one week of first dosing.
• Subjects who had used any investigational drug and/or participated in any clinical trial within 3 months of their first admission to this study.
• Subjects who had previously received BIA 3-202.
• Subjects who had donated and/or received any blood or blood products within the previous 2 months prior to screening.

Sponsors & Collaborators

• Bial - Portela C S.A.: lead

Study Sites (1)

Human Pharmacology Unit - BIAL - Portela & Ca, S.A.

S. Mamede Do Coronado, S. Mamede Do Coronado, 4745-457, Portugal

Location

MeSH Terms

Conditions

Parkinson Disease

Interventions

nebicapone

Condition Hierarchy (Ancestors)

Parkinsonian Disorders; Basal Ganglia Diseases; Brain Diseases; Central Nervous System Diseases; Nervous System Diseases; Movement Disorders; Synucleinopathies; Neurodegenerative Diseases

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 12, 2016
• First Posted: May 13, 2016
• Study Start: September 1, 2001
• Primary Completion: December 1, 2001
• Study Completion: December 1, 2001
• Last Updated: May 13, 2016

Record last verified: 2016-05

Data Sharing

• IPD Sharing: Will not share

Locations

PT (1)