In the Journal of Cystic Fibrosis, Santhera Pharmaceuticals (SIX: SANN) announces the online publication of information from Phase I with its human neutrophil elastase (hNE) inhibitor POL6014. POL6014 is an innovative, powerful and selective human neutrophil elastase (HNE) in the therapy of cystic fibrosis (CF) clinical development. In CF, excessive release of enzymes such as hNE accelerates inflammation and harm of the lung tissue, resulting in an incapacitating and progressive decrease in lung function. The two now released double-blind, placebo-controlled studies assessed the security, tolerability, and pharmacokinetics of single ascending doses of POL6014 in healthy volunteers and CF patients.
A total of 48 healthy volunteers and 24 CF patients were assigned randomly to different times of POL6014 or placebo in the two research. Healthy volunteers got POL6014 in doses ranging from 20 mg to 960 mg; 80 mg, 160 mg or 320 mg for CF patients definite decrease of active hNE in sputum was noted shortly after inhalation of POL6014 at all doses tested in CF patients. Also, sputum POL6014 concentrations for these patients appeared to be up to 1000-fold greater than plasma concentrations at 3 and 24 hours after inhalation, suggesting elevated lung exposure to POL6014 with very restricted systemic drug exposure. Doses of POL6014 up to 480 mg were considered safe and well-tolerated.
Based on the good Phase I data, Santhera is presently conducting a Phase Ib / IIa MAD (multiple ascending dose) research to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of various doses of POL6014 in oral inhalation in CF patients.
Santhera acquired Polyphor AG’s exclusive global rights to develop and market POL6014 in CF and other pulmonary diseases. With POL6014, the Cystic Fibrosis Foundation (CFF) provides financing for the behavior of safety tests.