Clinical Trials/NCT04991194

NCT04991194

Terminated

Phase 1

Effect of Age-gender on the Pharmacokinetic and Pharmacodynamic Profiles of BIA 5 1058. An Open-label, Parallel Group, Multiple Dose 10-day Study.

Bial - Portela C S.A.0 sites61 target enrollmentOctober 12, 2015

ConditionsPulmonary Arterial Hypertension

InterventionsBIA 5-1058

DrugsBIA 5-1058

Overview

Phase: Phase 1
Intervention: BIA 5-1058
Conditions: Pulmonary Arterial Hypertension
Sponsor: Bial - Portela C S.A.
Enrollment: 61
Primary Endpoint: Maximum observed plasma concentration (Cmax)
Status: Terminated
Last Updated: 4 years ago

Overview Investigators Eligibility Criteria Arms & Interventions Outcomes Similar Trials

Overview

Brief Summary

the purpose of this study is to determine the effect of age on the Pharmacokinetics (PK) profile of BIA 5-1058 at steady state after multiple oral doses

Detailed Description

This was a single-centre, open-label, parallel group, non-randomised, two-part multiple dose 10-day study in healthy young and elderly male and female subjects. The study comprised a screening evaluation between 2 and 28 days before the first Investigational Medicinal Product (IMP) administration, a hospitalisation period of 15 days comprising a treatment period of 10 days, and a follow-up visit approximately 7 days after discharge. Part 1: Subjects received 1200 mg of BIA 5-1058 once a day (od), in fasting conditions, for 10 days Part 2 : Subjects received 400 mg of BIA 5-1058 od, in fasting conditions, for 10 days.

Registry

clinicaltrials.gov

Start Date

October 12, 2015

End Date

December 30, 2016

Last Updated

4 years ago

Study Type

Interventional

Study Design

Parallel

Sex

All

Investigators

Sponsor

Bial - Portela C S.A.

Responsible Party

Sponsor

Eligibility Criteria

Inclusion Criteria

•All subjects (young and elderly):
•A signed and dated informed consent form before any study-specific screening procedure was performed;
•Healthy male and female subjects as determined by the Investigator on the basis of medical history, physical examination, clinical laboratory test results, vital signs and digital 12-lead electrocardiogram (ECG);
•Non-smoker or ex-smokers for at least 3 months at screening;
•BMI between 18 and 30 kg/m2, inclusive;
•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 the study;
•Negative screen for alcohol and drugs of abuse at screening and admission to the study;
•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.

Exclusion Criteria

•All subjects (young and elderly):
•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 \[1 unit corresponds to 1 glass of 12° wine (10 cL), 1 glass of 45° pastis (2.5 cL), 1 glass of 40° whisky (2.5 cL), 1 glass of 12° champagne (10 cL), 1 glass of 18°aperitif drink (7 cL) or one 25-cL glass of 5°beer\];
•Significant infection or known inflammatory process at screening or admission to study;
•Acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission to the study;
•Previous use of BIA 5-1058;
•Use of any investigational drug or participation in any clinical trial within 90 days prior to screening;

Arms & Interventions

BIA 5-1058 1200 mg (Part I)

Subjects received 1200 mg of BIA 5-1058 once a day (od), in fasting conditions, for 10 days

Intervention: BIA 5-1058

BIA 5-1058 400 mg (Part II)

Subjects received 400 mg of BIA 5-1058 od, in fasting conditions, for 10 days.

Intervention: BIA 5-1058

Outcomes

Primary Outcomes

Maximum observed plasma concentration (Cmax)

Time Frame: Up to 4 weeks

Pharmacokinetic analysis Blood samples for PK analysis were taken at the following times: On D1: before BIA 5-1058 dosing (pre-dose), and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16 and 24 h post-dose (before the second administration on D2). On D3, D7, D8 and D9: before BIA 5-1058 dosing. From D10 to D13: before BIA 5-1058 dosing, and 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24 (D11), 36 (D11), 48 (D12), 60 (D12) and 72h post-dose (D13).

Time of occurrence of Cmax (tmax)

Time Frame: Up to 4 weeks

Area under the plasma concentration-time curve from time zero to 24 hours after last dosing (AUC0-24)

Time Frame: Up to 4 weeks

Apparent total body clearance (CL/F)

Time Frame: Up to 4 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-t)

Time Frame: Up to 4 weeks

Apparent terminal half-life (t½)

Time Frame: Up to 4 weeks