How does BAY85-8501 work?
Preclinical studies demonstrate that BAY85-8501 works by inhibiting the human neutrophil elastase (HNE) in the lung, improving lung inflammation.
Human neutrophil elastase is an enzyme with an important role in tissue inflammation. Research has found that lung diseases such as bronchiectasis, COPD and pulmonary hypertension development and progression is due to an excess of human neutrophil elastase activity.
A Phase 2a study (NCT01818544) assessed the safety and efficacy of 28 days of oral administration of 1 mg of BAY85-8501 once daily, against a placebo, in 94 people with non-CF bronchiectasis. The study’s primary objectives included the number of participants who needed to stop the treatment, changes in blood pressure, heart rate and ECG, and the number of treated patients with altered liver blood markers.
Secondary objectives included changes in lung function as measured by the FEV1 and FVC, changes in the quality of life as measured by the St. Georges Respiratory Questionnaire (SGRQ), changes in sputum weight, and biomarkers and blood biomarkers of inflammation and tissue damage change.
Results showed that placebo as well as treated patients, in almost equal numbers, reported treatment-emergent adverse events (TEAEs). Of the 67 patients patients reporting these events, 31 were treated with BAY85-8501 and 36 received placebo. The most frequent TEAEs were headache, and cold-like symptoms and cough.
No clinically relevant changes in blood pressure, heart rate, ECG or blood parameters were recorded. Compared to placebo, there also were no significant changes in lung function, quality of life, 24-hour sputum weight, and neutrophil elastase activity and concentration or other biomarkers.
The administration of 1 mg of BAY85-8501 was considered safe and well-tolerated and supported once-a-day dosing. Further studies were recommended.
Earlier bioavailability and food effect studies showed that both tablet and solution of BAY85-7501 formulation had satisfactory pharmacokinetics, with comparable bioavailability and that although food intake decreased the absorption rate, it did not affect its extent.
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