Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
To determine the basic pharmacokinetics of BI 1356 BS, its metabolite CD 1750 XX and radioactivity including excretion mass balance, excretion pathways and metabolism following the intravenous and oral administration of [14C] BI 1356 BS
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Label | Type | Description | Intervention Names |
|---|---|---|---|
| [14C] BI 1356 as oral (p.o.) solution | Experimental |
| |
| [14C] BI 1356 solution for i.v. infusion | Experimental |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| [14C] BI 1356 as oral (p.o.) solution | Drug |
| ||
| [14C] BI 1356 solution for i.v. infusion |
| Measure | Description | Time Frame |
|---|---|---|
| Comparison of individual time course profiles of [14C] radioactivity in whole blood, plasma, urine and faeces | before and up to 264 h after drug administration | |
| Comparison of individual time course profiles of BI 1356 BS and its metabolite CD 1750 XX in plasma and urine | before and up to 264 h after drug administration | |
| Rate and extent of excretion mass balance based on the total radioactivity in urine and faeces | prior to and up to 120 h after start of administration | |
| CBlood cell/Cplasma ratio of [14C] -radioactivity | 1:30, 3, 24 and 72 h after drug administration | |
| Measurement of the plasma protein binding of total [14C] radioactivity in human plasma samples ex vivo | 1:30 and 3 hours post drug administration | |
| Cmax (maximum concentration of the analyte(s) in plasma) | before and up to 264 h after drug administration | |
| tmax (time from dosing to the maximum concentration of the analyte(s) in plasma) | before and up to 264 h after drug administration | |
| AUC0-tz (area under the concentration-time curve of the analyte(s) in plasma over the time interval from 0 to the time of the last quantifiable data point) | before and up to 264 h after drug administration | |
| AUC0-infinity (area under the concentration-time curve of the analyte(s) in plasma over the time interval from 0 to infinity) |
| Measure | Description | Time Frame |
|---|---|---|
| Number of patients with adverse events | up to 47 days | |
| Global assessment of tolerability by investigator on a 4-point scale | on day 12 during ambulant visit or on day of discharge on day 13, 14 or 15 |
Not provided
Inclusion Criteria:
- Healthy males according to the following criteria: Based upon a complete medical history, including the physical examination, vital signs Blood Pressure (BP), Pulse Rate (PR)), 12-lead Electrocardiogram (ECG), clinical laboratory tests
Exclusion Criteria:
Exclusion criteria specific for this study:
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Drug |
|
| before and up to 264 h after drug administration |
| λz (terminal rate constant in plasma) | before and up to 264 h after drug administration |
| t1/2 (terminal half-life of the analyte(s) in plasma) | before and up to 264 h after drug administration |
| MRTpo and MRT, respectively (mean residence time of the analyte(s) in the body after p.o. and i.v. administration) | before and up to 264 h after drug administration |
| CL/F (apparent/total clearance of the analyte(s) in plasma following extravascular and intravenous administration) | before and up to 264 h after drug administration |
| Vz/F (apparent volume of distribution during the terminal phase λz following an extravascular or intravenous administration (F=1) respectively) | before and up to 264 h after drug administration |
| feurine,0-tz (amount of analyte excreted in urine within the time interval zero to tz (=120 h) in % of dose) | prior to and up to 120 h after start of administration |
| fefaeces,0-tz (amount of analyte excreted in faeces within the time interval zero to tz (=120 h) in % of dose) | up to 120 h after drug administration |
| CLR,0-tz (renal clearance of analyte) | prior to and up to 120 h after start of administration |
| Fa (drug absorption based on radioactivity data) | up to 264 h after drug administration |
| Evaluation of local tolerability of the infusion by investigator on a 6-point scale | after start of infusion up to day 15 |
| ID | Term |
|---|---|
| D000069476 | Linagliptin |
| D012996 | Solutions |
| ID | Term |
|---|---|
| D011687 | Purines |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| D006571 | Heterocyclic Compounds |
| D011799 | Quinazolines |
| D004364 | Pharmaceutical Preparations |
Not provided
Not provided