Absorption, Distribution, Metabolism and Excretion of [14C] Labelled BIA 5-1058

• Status: Completed
• Trial end date: 2019-05-02
• Target enrollment: 0
• Participant gender: Male

Summary

The purpose of the study is to determine the mass balance recovery in expired air, urine and faeces after a single oral dose of 400 mg 14C-labeled BIA 5-1058; to provide plasma, urine and faecal samples for metabolite profiling and structural identification; and determine the routes and rates of elimination of [14C]-BIA 5-1058

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

Details

• Lead Sponsor: Bial - Portela C S.A.

Criteria

Inclusion Criteria:

• Healthy males;

• Age 30 to 65 years of age, inclusive;

• Body mass index (BMI) of 18.0 to 32.0 kg/m2, inclusive;

• Normal resting supine BP (Systolic BP: 90-140 mmHg [age 18-45] 90 160 mmHg [age >45], Diastolic BP: 40-90 mmHg) and heart rate: 40-90 bpm (age 18-45) 50-90 bpm (age >45) or showing no clinically relevant deviation as judged by the investigator or delegate;

• Digital (12-lead) ECG recording without signs of clinically relevant pathology or showing no clinically relevant deviations as judged by the investigator or delegate;

• All values for clinical laboratory tests of blood and urine within the normal range or showing no clinically relevant deviations as judged by the investigator or delegate;

• Must be willing and able to communicate and participate in the whole study;

• Must have regular bowel movements (ie, average stool production of between ≥1 every 2 days and ≤3 stools per day);

• Must provide written informed consent;

• Must agree to adhere to the contraception requirements

Exclusion Criteria:

• Females;

• Subjects who have received any IMP in a clinical research study within the previous 90 days prior to Day 1 of the study;

• Subjects who are study site employees, or immediate family members of a study site or sponsor employee;

• Subjects who have previously received BIA 5-1058 (including participation in QCL118167);

• History of any drug or alcohol abuse in the past 2 years;

• Regular alcohol consumption in males >21 units per week (1 unit = ½ pint beer, or a 25 mL shot of 40% spirit, 1.5 to 2 Units = 125 mL glass of wine, depending on type);

• Current smokers and those who have smoked within the last 12 months. A breath carbon monoxide reading of greater than 10 ppm at screening and admission;

• Current users of e-cigarettes and nicotine replacement products and those who have used these products within the last 12 months;

• Radiation exposure, including that from the present study, excluding background radiation but including diagnostic x-rays and other medical exposures, exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years. No occupationally exposed worker, as defined in the Ionising Radiation Regulations 2017, shall participate in the study;

• Subjects who do not have suitable veins for multiple venepunctures/cannulation as assessed by the investigator at screening;

• Clinically significant abnormal biochemistry, haematology or urinalysis as judged by the investigator (laboratory parameters are listed in Appendix 2);

• Positive drugs of abuse test result;

• Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) results;

• An estimated creatinine clearance of <90 mL/min based on creatinine clearance calculation using the Cockcroft-Gault equation and normalised to an average surface area of 1.73 m2;

• Clinically significant history of cardiovascular, renal, hepatic, respiratory and particularly GI disease, especially peptic ulceration, GI bleeding, ulcerative colitis, Crohn's Disease or Irritable Bowel Syndrome, as judged by the investigator or sub investigator;

• Frequent headaches and/or migraine, recurrent nausea, and/or vomiting (more than twice a month);

• Serious adverse reaction or serious hypersensitivity to any drug or the formulation excipients;

• Presence or history of clinically significant allergy requiring treatment, as judged by the investigator. Hay fever is allowed unless it is active;

• Donation or loss of greater than 400 mL of blood within the previous 3 months;

• Subjects who are taking, or have taken, any prescribed or over-the-counter drug (other than 2 g paracetamol per day) or herbal remedies in the 14 days before IMP administration. Exceptions may apply on a case by case basis, if considered not to interfere with the objectives of the study, as agreed by the PI and sponsor's medical monitor;

• Failure to satisfy the investigator of fitness to participate for any other reason.