Journal
EXPERT OPINION ON THERAPEUTIC PATENTS
Volume 23, Issue 10, Pages 1383-1389Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1517/13543776.2013.829454
Keywords
airway rehydration; amiloride; cystic fibrosis; epithelial sodium channel; mucociliary clearance
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Funding
- German Study Foundation
- German Research Foundation (DFG) [AL1453/1-1, AL1453/1-2]
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Novel molecular platforms for epithelial sodium channel (ENaC) modulators are claimed in the following six patents: WO2012035158(A1); WO2009074575 (A2); WO2011028740(A1); WO2009150137(A2); WO2011079087(A1); WO2008135557(A1). These ENaC inhibitors may be used in blocking transepithelial sodium and consequently water absorption across airway epithelia. This may result in airway rehydration and enhanced mucociliary clearance in patients with cystic fibrosis (CF) lung disease. All inhibitors resemble the classical ENaC blocker amiloride but follow different strategies to increase structural diversity in a sterically tolerant region. These substitutions can be modified to i) enhance potency of ENaC inhibition; ii) reduce epithelial permeability; and iii) broaden applicability in order to be used as potential drugs for CF therapy. Most of the claims and patent data are supported by the currently available literature. The patents deliver a solid chemical basis for a variety of chemical modifications of the ENaC inhibitor amiloride. These modifications may result in the development of a novel, applicable ENaC inhibitors which may have lasting effects on diseased airways and may achieve airway rehydration and enhanced mucociliary clearance in CF lung disease.
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