Phase I Multiple dose escalation study
Primary objective: To investigate the safety and tolerability of BAY 94-8862 after multiple oral doses of 10 mg twice a day (bid), 20 mg bid and 40 mg once a day given as 10 mg immediate release tablets over 10 days in 12 healthy male subjects (9-verum and 3 placebo) per dose step in a randomized, single-blind, placebo-controlled, group-comparison design.
Secondary objectives: To assess
- The pharmacodynamics of BAY 94-8862 and pharmacokinetics (PK) of BAY 94-8862 and three metabolites
- The influence of multiple oral doses of BAY 94-8862 given as 20 mg bid over 10 days on the PK of a single oral dose of the CYP3A4 substrate midazolam in 9 healthy male subjects.
- Healthy male white subjects, 18 to 45 years of age, body mass index ( ≥ 18.0 and ≤ 29.9 kg/m²
- Subjects with conspicuous findings in medical history and pre-study examination - Recent donation of blood/blood components - Clinically relevant changes/deviations from normal electrocardiography, physical examination, clinical chemistry, hematology, urinalysis, and/or blood pressure, heart rate (vital signs) - Regular daily consumption of an amount of beer, alcohol, xanthine-containing beverages, foods or beverages containing grapefruit and/or cigarettes that may affect study results - History of/current relevant diseases of vital or other organs and of the central nervous system and/or medical conditions that would impair subject’s ability to participate in the trial or that may affect study results - Subjects with a history of severe allergies, non-allergic drug reactions, or multiple drug allergies or with hypersensitivity to the investigational drugs, the control agent and/or to inactive constituents - Regular use of therapeutic or recreational drugs - Use of medication within the 2 weeks preceding the study, especially concomitant administration of potassium-sparing diuretics, ACE inhibitors, angiotensin-II-receptor blockers, potassium or calcium supplements, nonsteroidal anti-inflammatory drugs like acetylsalicylic acid, indomethacin or ibuprofen, concomitant use of strong CYP3A4 inducers and inhibitors, weak to moderate CYP3A4 inhibitors - Subjects testing positive in the drug screening - Subject testing positive for human immunodeficiency virus type 1 and 2 antibody, hepatitis B surface antigen or hepatitis C virus antibody - Serum potassium level greater than equal to 5.0 mmol/L, serum sodium level less than equal to 130 mmol/L - History of myasthenia gravis, narrow angle glaucoma - Known sleep apnea syndrome - Known hereditary galactose intolerance, lactase deficiency or glucose-galactase deficiency - Regular intake of liquorice or intake of liquorice within the last 14 days prior study treatment
Wuppertal, Germany, 42096
E-mail: [email protected]
Phone: (+)1-888-84 22937
Multiple dose basic phase I dose escalation study, to investigate safety, tolerability, pharmacokinetics and pharmacodynamics of BAY 94-8862 after oral dosing of 10 mg bid, 20 mg bid or 40 mg od over 10 days given as 10 mg IR-tablets in 12 healthy male subjects per dose step in a randomized, single-blind, placebo-controlled, group-comparison design