Safety, Tolerability and Pharmacokinetics of BEA 2180 BR in Healthy Male Volunteers

A Randomised, Single-blind, Placebo-controlled (Within Dose Groups) Study to Assess Safety, Tolerability and Pharmacokinetics of Single Rising Intravenous Doses (2.5 μg, 7.5 μg, 25 μg, 50 μg, 100 μg, 200 μg, 350 μg, 500 μg Free Cation) BEA 2180 BR in Healthy Male Volunteers With an Additional Arm by Inhalation in One Dose Group (1600 μg)

Evaluation of safety, tolerability and pharmacokinetics of single rising intravenous doses of BEA 2180 BR; additional exploration of metabolism following inhalation

Inclusion Criteria:

1. Healthy male based upon a complete medical history, including the physical examination, regarding vital signs (BP, PR), 12 lead ECG measurement, and clinical laboratory tests. There is no finding deviating from normal and of clinical relevance. There is no evidence of a clinically relevant concomitant disease.
2. Age ≥21 and ≤50 years
3. BMI ≥18.5 and <29.9 kg/m2 (Body Mass Index)
4. Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice (GCP) and the local legislation.

Exclusion Criteria:

1. Any finding of the medical examination (including blood pressure (BP), pulse rate (PR), and ECG measurements) deviating from normal and of clinical relevance

2. Evidence of a clinically relevant concomitant disease

3. Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders

4. Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders

5. History of relevant orthostatic hypotension, fainting spells or blackouts

6. Chronic or relevant acute infections

7. History of relevant allergy/hypersensitivity (including allergy to the drug or its excipients) as judged clinically relevant by the investigator

8. Intake of drugs with a long half-life (>24 hours) within at least 1 month or less than 10 half-lives of the respective drug prior to randomisation

9. Use of drugs which might reasonably influence the results of the trial based on the knowledge at the time of protocol preparation within 10 days prior to enrolment in the study or during the study

10. Participation in another trial with an investigational drug within 2 months prior to randomisation

11. Smoker (>10 cigarettes or >3 cigars or >3 pipes/day)

12. Inability to refrain from smoking on trial days as judged by the investigator

13. Alcohol abuse (regularly more than 40 g alcohol per day for men)

14. Drug abuse

15. Blood donation (more than 100 mL blood within 4 weeks prior to randomisation or during the trial)

16. Excessive physical activities within 1 week prior to randomisation or during the trial

17. Any laboratory value outside the reference range that is of clinical relevance

18. Inability to comply with dietary regimen of the study centre

    The following exclusion criteria are specific for this study due to the known class side effect profile of anticholinergic drugs:

19. hypersensitivity to tiotropium and/or related drugs of these classes

20. history of narrow-angle glaucoma

21. history of prostatic hyperplasia

22. history of bladder-neck obstruction