Effect of Food on BIA 5-1058

NCT04991155 | Completed Phase 1

• 2 other identifiers: BIA-51058-1022015-001951-65
• Study Type: interventional
• Target: 57
• Locations: 0 countries
• Sites: N/A

Brief Summary

The aim of this study is to investigate the effect of food on the pharmacokinetic (PK) profile of BIA 5-1058 after a single dose in healthy subjects.

Conditions

Pulmonary Arterial Hypertension

Outcome Measures

Primary Outcomes (4)

• Maximum observed plasma concentration (Cmax)

  In all treatment periods, blood samples were taken at the following times: before BIA 5-1058 dosing, and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose

  Up to 9 weeks

• Time of occurrence of Cmax (tmax)

  In all treatment periods, blood samples were taken at the following times: before BIA 5-1058 dosing, and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose

  Up to 9 weeks

• Area under the plasma concentration-time curve (AUC)

  In all treatment periods, blood samples were taken at the following times: before BIA 5-1058 dosing, and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose

  Up to 9 weeks

• Area under the plasma concentration-time curve (AUC) from time zero to the last sampling time at which the drug concentration was at or above the lower limit of quantification (AUC0-last)

  In all treatment periods, blood samples were taken at the following times: before BIA 5-1058 dosing, and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 60 and 72 h post-dose

  Up to 9 weeks

Study Arms (3)

PART 1 (400 mg BIA 5-1058)

EXPERIMENTAL

Each subject was orally administered a single oral dose of BIA 5-1058 on D1 (dosing day) on three different occasions (Period 1, Period 2 and Period 3): Part 1: 400 mg BIA 5-1058 as four (4) 100 mg tablets in Period 1, 400 mg BIA 5-1058 as four (4) 100 mg tablets in Period 2, and 400 mg BIA 5-1058 as four (4) 100 mg tablets in Period 3.

Drug: BIA 5-1058

PART 2 (800 mg BIA 5-1058)

EXPERIMENTAL

Each subject was orally administered a single oral dose of BIA 5-1058 on D1 (dosing day) on three different occasions (Period 1, Period 2 and Period 3): Part 2: 800 mg BIA 5-1058 as eight (8) 100 mg tablets in Period 1, 800 mg BIA 5-1058 as eight (8) 100 mg tablets in Period 2, and 800 mg BIA 5-1058 as eight (8) 100 mg tablets in Period 3.

Drug: BIA 5-1058

PART 3 (1200 mg BIA 5-1058)

EXPERIMENTAL

Each subject was orally administered a single oral dose of BIA 5-1058 on D1 (dosing day) on three different occasions (Period 1, Period 2 and Period 3): Part 3: 1200 mg BIA 5-1058 as twelve (12) 100 mg tablets in Period 1, 1200 mg BIA 5-1058 as twelve (12) 100 mg tablets in Period 2, and 1200 mg BIA 5-1058 as twelve (12) 100 mg tablets in Period 3.

Drug: BIA 5-1058

Interventions

BIA 5-1058 DRUG

BIA 5-1058 (tablets 100 mg) was administered orally with 240 mL (Part 1) or 270 mL (Part 2 and Part 3) of water, in one period in the morning under fasting conditions (after at least a 10-hour overnight fast), in one period in the morning after a moderate meal, and in the other period at lunch after a moderate meal.

Also known as: Zamicastat

PART 1 (400 mg BIA 5-1058); PART 2 (800 mg BIA 5-1058); PART 3 (1200 mg BIA 5-1058)

Eligibility Criteria

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

You may qualify if:

• Able and willing to give written informed consent and to comply with the study restrictions;
• Male or 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, complete neurological examination and 12-lead electrocardiogram (ECG);
• Negative tests for hepatitis B surface antigen (HBsAg), anti-hepatitis C virus antibodies (HCV Ab) and anti-human immunodeficiency virus antibodies (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 for at least 3 months.
• If female:
• No childbearing potential by reason of surgery or at least 1 year post menopause (i.e., 12 months post last menstrual period), or menopause confirmed by follicle-stimulating hormone (FSH) testing;
• If of childbearing potential, she was using an effective non-hormonal method of contraception \[intrauterine device or intrauterine system; condom or occlusive cap (diaphragm or cervical or vault caps) with spermicidal foam or gel or film or cream or suppository; true abstinence; or vasectomized male partner, provided that he is the sole partner of that subject\] for all the duration of the study;
• Negative serum pregnancy test at screening and negative urine pregnancy test on admission of each treatment period (women of childbearing potential only).
• If male:
• Using an effective method of contraception with a pregnant partner or partner of childbearing potential (condom or occlusive cap \[diaphragm or cervical or vault caps\] with spermicidal foam or gel or film or cream or suppository; true abstinence; or vasectomy) throughout the study;
• Refraining from donating sperm throughout the study.

You may not qualify if:

• 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;
• Clinically relevant surgical history;
• History of relevant atopy or drug hypersensitivity;
• History of alcoholism or drug abuse;
• Consumption of more than 14 units of alcohol a week \[1 glass (25 cL) of beer with 3° of alcohol = 7.5 g, or 1 glass (25 cL) of beer with 6° of alcohol = 15 g, or 1 glass (12.5 cL) of wine with 10° of alcohol = 12 g, or 1 glass (4cL) of aperitif with 42° of alcohol = 17 g\];
• Significant infection or known inflammatory process at screening or admission to each treatment period;
• Display of acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission to each treatment period;
• Use of medicines within 2 weeks of admission to the first period that may could affect the safety or other study assessments, in the Investigator's opinion;
• Previous administration of BIA 5-1058;
• Use of any investigational drug or participation in any clinical trial within 90 days prior to screening;
• Participation in more than 2 clinical trials within the 12 months prior to screening;
• Donation or reception of any blood or blood products within the 3 months prior to screening;
• Vegetarians, vegans or had any other medical dietary restrictions;
• Not able to communicate reliably with the Investigator;
• Unlikely to co-operate with the requirements of the study.

Sponsors & Collaborators

• Bial - Portela C S.A.: lead

MeSH Terms

Conditions

Pulmonary Arterial Hypertension

Interventions

zamicastat

Condition Hierarchy (Ancestors)

Hypertension, Pulmonary; Lung Diseases; Respiratory Tract Diseases

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 28, 2021
• First Posted: August 5, 2021
• Study Start: July 20, 2015
• Primary Completion: September 22, 2015
• Study Completion: September 22, 2015
• Last Updated: August 5, 2021

Record last verified: 2021-07

Data Sharing

• IPD Sharing: Will not share