The primary objective of this trial was to assess the safety and tolerability of BIBF 1120 administered as intravenous (iv) infusions of 1, 3, 10, and 20 mg, and to assess the absolute bioavailability of orally administered 100 mg BIBF 1120 as soft gelatine capsules. A secondary objective was the exploration of the pharmacokinetic (PK) of BIBF 1120 after single iv dosing, including dose proportionality.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
SINGLE
Enrollment
30
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞)
Time frame: Up to 48 hours after drug administration
Area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the time of the last quantifiable data point (AUC0-tz)
Time frame: Up to 48 hours after drug administration
Maximum measured concentration of the analyte in plasma (Cmax)
Time frame: Up to 48 hours after drug administration
Time from dosing to the maximum concentration of the analyte in plasma (tmax)
Time frame: Up to 48 hours after drug administration
%AUCtz-∞ (calculated from AUC0-∞ and AUC0-tz )
Time frame: Up to 48 hours after drug administration
Terminal rate constant in plasma (λz)
Time frame: Up to 48 hours after drug administration
Terminal half-life of the analyte in plasma (t1/2)
Time frame: Up to 48 hours after drug administration
Mean residence time of the analyte in the body after oral administration (MRTpo)
Time frame: Up to 48 hours after drug administration
Mean residence time of the analyte in the body after iv administration (MRT)
Time frame: Up to 48 hours after drug administration
Apparent clearance of the analyte in plasma after extravascular administration (CL/F)
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Time frame: Up to 48 hours after drug administration
Apparent clearance of the analyte in plasma after intravenous administration (CL)
Time frame: Up to 48 hours after drug administration
Apparent volume of distribution during the terminal phase λz following an extravascular dose (Vz/F)
Time frame: Up to 48 hours after drug administration
Apparent volume of distribution during the terminal phase λz following an intravenous dose (Vz)
Time frame: Up to 48 hours after drug administration
Apparent volume of distribution at steady-state following an intravenous dose (Vss)
Time frame: Up to 48 hours after drug administration
Amount of analyte that is eliminated in urine within the time interval t1 to t2 (Aet1-t2)
Time frame: Up to 48 hours after drug administration
Fraction of analyte excreted in urine within the time interval t1 to t2, in percentage of dose (fet1-t2)
Time frame: Up to 48 hours after drug administration
Renal clearance of analyte within the time interval t1 to t2 (CLR,t1-t2)
Time frame: Up to 48 hours after drug administration
Change from baseline in physical examination
Time frame: Baseline, day 46
Change from baseline in vital signs (BP, PR)
Time frame: Baseline, day 46
Change from baseline in 12-lead ECG (electrocardiogram)
Time frame: Baseline, day 46
Change from baseline in clinical laboratory test (hematology, clinical chemistry and urinalysis)
Time frame: Baseline, day 46
Number of Participants with Serious and Non-Serious Adverse Events
Time frame: Up to day 46
Assessment of tolerability by investigator on a four point scale (good, satisfactory, not satisfactory, bad)
Time frame: Up to day Day 46