Safety, Tolerability, Pharmacokinetic, Including Food Interaction, and Pharmacodynamic Profile of BIA 5-1058.

• Status: Completed
• Trial end date: 2012-01-01
• Target enrollment: 0
• Participant gender: Male

Summary

The purpose of this study is to to assess the safety and tolerability of BIA 5 1058 after single and multiple oral doses

• Phase: Phase 1
• Accepts Healthy Volunteers?: Accepts Healthy Volunteers

Details

• Lead Sponsor: Bial - Portela C S.A.
• Treatments: Zamicastat

Criteria

Inclusion Criteria:

Subjects were eligible for the study if they met all the following inclusion criteria:

• Gender - male

• Age - 18 - 55 years, inclusive

• Body Mass Index (BMI) - 18.0 - 30.0 kg m2 (BMI (kg m2) = Body weight (kg) - Heigh t2 (m 2))

• Ability and willingness to abstain from alcohol, methylxanthine-containing beverages or food (coffee, tea, cola, chocolate, power drinks), grapefruit (juice) and tobacco products from 48 h prior to entry in the clinical research centre until discharge

• Medical history without major pathology

• Normal resting supine blood pressure and pulse rate showing no clinically relevant deviations as judged by the MI

• Computerised (12-lead) ECG recording without signs of clinically relevant pathology or showing no clinically relevant deviations as judged by the MI

• All values for haematology and for clinical chemistry tests of blood and urine within the normal range or showing no clinically relevant deviations as judged by the MI

• Willingness to sign the written ICF

Exclusion Criteria:

Subjects were excluded from participation if any of the following exclusion criteria applied

• Any significant cardiovascular (e.g. hypertension), hepatic, renal, respiratory (e.g. childhood asthma), gastrointestinal, endocrine (e.g. diabetes, dyslipidemia), immunologic, haematological, neurologic, or psychiatric disease

• An automatic ECG QTc interval reading at screening or enrolment of + 440 ms.

• Evidence of clinically relevant pathology

• Mental handicap

• History of relevant drug and or food allergies

• Smoking more than 10 cigarettes and or cigars and or pipes daily

• History of alcohol abuse or drug addiction (including soft drugs like cannabis products)

• Use of any prescription drug within 30 days before study drug administration with the exception of influenza vaccination

• Use of any over-the-counter drugs including health supplements, herbal supplements such as St. John's Wort extract (except for the occasional use of acetaminophen (paracetamol), aspirin and vitamins - 100 recommended daily allowance) within 7 days before study drug administration. The use of paracetamol and or topical medication was allowed up to 3 days before entrance into the clinical research facility

• Participation in a drug study within 90 days prior to drug administration

• Participation in more than 3 other drug studies in the 10 months preceding the start of this study (this was the first administration of study drug)

• Donation of more than 50 mL of blood within 90 days prior to first drug administration

• Donation of more than 1.5 litres of blood in the 10 months preceding the start of this study (this was the first administration of study drug)

• Positive screen on drugs of abuse (opiates, methadone, cocaine, amphetamines, cannabinoids), barbiturates, benzodiazepines, tricyclic antidepressants and alcohol

• Intake of more than 24 units of alcohol per week (1 unit of alcohol equals approximately 250 mL of beer, 100 mL of wine or 35 mL of spirits)

• Positive screen on hepatitis B surface antigen (HBsAg)

• Positive screen on anti hepatitis C virus (HCV)

• Positive screen on anti human immunodeficiency virus (HIV) 1 - 2

• Acute disease state indicated as clinically relevant by the MI (e.g. nausea, vomiting, fever, diarrhoea) within 7 days before the first drug administration

• Non-willingness to consume the Food and Drug Administration (FDA) breakfast (FE part only)