This study is a randomized, double-blind, placebo-controlled, single ascending dose study to evaluate safety, tolerability, and pharmacokinetics of single doses of BTZ043 in healthy adult volunteers. The study is conducted at a study centre in Germany. Up to 50 male and female participants will be included in this study in up to 5 cohorts; each cohort will consist of 10 subjects: in each cohort 8 subjects will be assigned to BTZ-043 and 2 to placebo. The doses tested will be: 125mg, 250mg, 500mg, 1000mg and 2000mg. Safety will be assessed via regular vital sign measurement, 12-lead ECG parameters, physical examination and safety laboratory assessments. Subjects will be hospitalized from Day -1 until discharge in the morning of Day 3. After completion of all Day 3 assessments of a cohort, blinded safety data will be reviewed and the next dose increment will be decided by the Trial Steering Committee (TSC).
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
QUADRUPLE
Enrollment
30
Nuvisan
Neu-Ulm, Bavaria, Germany
Number of participants with treatment-related adverse events concerning ECG as assessed by CTCAE v4.03 (Common Terminology Criteria for Adverse Events)
Measured by 12-lead ECG assessments on 6 different timepoints.
Time frame: 0.5 hours to 12.0 hours post-dosing
Number of participants with treatment-related adverse events concerning safety laboratory as assessed by CTCAE v4.03
Measured by clinical chemistry, haematology, coagulation, urinalysis on 2 different timepoints
Time frame: 24 hours to 26 hours post-dosing
Number of participants with treatment-related adverse events concerning vital signs as assessed by CTCAE v4.03
Measured by blood pressure, pulse rate, respiratory rate and tympanic body temperature on 7 different timepoints
Time frame: 0.25 hours to 48 hours post-dosing
Number of participants with treatment-related adverse events concerning clinical observations as assessed by CTCAE v4.03
Examination of general appearance, skin, neck (including thyroid), throat, lungs, heart, abdomen, back, lymph nodes, extremities, vascular and neurological systems.
Time frame: 4 hours to 48 hours post-dosing
Pharmacokinetic assessment of BTZ-043 after a single oral dose
Blood samples for the determination of Area under the plasma concentration versus time curve (AUC) will be assessed in BTZ-043 and the metabolites BTZ-045S and M2
Time frame: 0.25 hours to 36 hours post-dosing
Pharmacokinetic assessment of BTZ-043 after a single oral dose
Blood samples for the determination of Peak Plasma Concentration (Cmax) will be assessed in BTZ-043 and the metabolites BTZ-045S and M2
Time frame: 0.25 hours to 36 hours post-dosing
Determining the effect of sex differences on systemic exposure by analyzing the PK of BTZ-043 in male and female participants.
Estimated via comparison of the exposure (AUC0-inf) of BTZ-043 in males and females
Time frame: 0.25 hours to 36 hours post-dosing
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