Effect of BIA 5-1058 400 mg on Warfarin Pharmacokinetics (NCT04994119) | Clinical Trial Compass
CompletedPhase 1
Effect of BIA 5-1058 400 mg on Warfarin Pharmacokinetics
Germany26 participantsStarted 2018-02-23
Plain-language summary
The purpose of this study is:
* To investigate CYP2C9 inhibition by BIA 5-1058 through the assessment of its effect on the Pharmacokinetic (PK) of S-warfarin, a substrate of CYP2C9.
* To assess the effect of warfarin on the PK of BIA 5-1058.
Who can participate
Age range18 Years – 45 Years
SexALL
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AI-rewrites the medical criteria so a patient or caregiver can understand them. Always confirm with the trial site.
Inclusion criteria
✓. Provided signed and dated informed consent before any study specific procedures were conducted.
✓. Male and female subjects aged 18 to 45 years (both inclusive) at the Screening Visit.
✓. Healthy as determined by the Principal Investigator on the basis of medical history, physical examination, clinical laboratory test results, vital signs and digital 12 lead electrocardiogram (ECG). If a vital sign or ECG assessment was outside of the reference range at the Screening Visit or baseline, the assessment could have been repeated once as soon as possible and in any cases before enrollment to rule out any error.
✓. Non-smoker or ex-smoker for at least 3 months prior to the Screening Visit.
✓. Body mass index (BMI) between 18.5 and 29.9 kg/m2 (both inclusive) at the Screening Visit and on admission to each treatment period.
✓. Negative test results for hepatitis B surface antigen (HBsAg), hepatitis B core antibody (anti HBc), immunoglobulin M (IgM) anti-HBc, hepatitis C virus antibody (anti HCV) and human immunodeficiency virus (HIV) (Types 1 and 2) antibodies at the Screening Visit.
✓. Negative screen for alcohol and drugs of abuse at the Screening Visit and on admission to each treatment period.
✓. Subject had to be willing and able to be confined to the clinical unit and had to adhere to the study and lifestyle restrictions.
Exclusion criteria
✕. Clinically relevant history or presence of respiratory, gastrointestinal, renal, hepatic, hematological, lymphatic, neurological, cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological, dermatological, endocrine, connective tissue disease or disorders within 5 years before the first investigational medicinal product (IMP) administration.
What they're measuring
1
Cmax - Maximum observed concentration
Timeframe: Up to 2 months and 2 weeks
2
AUC0-t - Area under the plasma concentration-time curve (AUC) from time zero to the last quantifiable concentration
Timeframe: Up to 2 months and 2 weeks
3
AUC0-inf - AUC from time zero extrapolated to infinity
✕. Documented coronary artery disease (any of prior myocardial infarction, positive stress test, positive nuclear perfusion study, prior coronary artery bypass graft \[CABG\] surgery or percutaneous coronary intervention, angiogram showing at least 75% stenosis in a major coronary artery), acute coronary syndrome or current symptoms of myocardial ischemia and angina.
✕. Clinically relevant surgical history involving the stomach and/or intestinal system, potentially affecting absorption of IMPs.
✕. Any clinically relevant findings in the laboratory tests, particularly any abnormality in the coagulation tests or the liver function tests, as judged by the Principal Investigator, at the Screening Visit and on admission to each treatment period. If a laboratory assessment was outside of the reference range at the local laboratory at the Screening Visit or baseline, the assessment could have been repeated once as soon as possible and in any cases before enrolment to rule out laboratory error.
✕. Subjects with alanine aminotransferase (ALT) \> 1.0 x the upper limit of normal (ULN) and/or aspartate aminotransferase (AST) \> 1.0 x ULN and/or total bilirubin \> 1.0 x ULN (isolated bilirubin \> 1.0 x ULN and 1.5 x ULN was acceptable if bilirubin was fractionated and direct bilirubin \< 35%), as confirmed by subsequent repeat assessment, at the Screening Visit and on admission to each treatment period.
✕. History of relevant atopy or drug hypersensitivity.
✕. History of alcoholism or drug abuse.
✕. History of drinking \> 24 g (males) and \> 12 g (females) of pure alcohol per day (10 g pure alcohol = 250 mL of beer \[5%\] or 35 mL of spirits \[35%\] or 100 mL of wine \[12%\]) within 3 months before first admission to the clinical unit.