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Advances in treatment of pulmonary arterial hypertension: patent review
Authors:Bhuvaneshwar Vaidya  Matthew Pangallo  Gregoire Ruffenach  Christine Marie Cunningham  Jeanette C Perron  Srikanth Kolluru
Institution:1. School of Pharmacy, Keck Graduate Institute, Claremont, CA, USA;2. School of Applied Life Sciences, Keck Graduate Institute, Claremont, CA, USA;3. Division of Molecular Medicine, Department of Anesthesiology, David Geffen School of Medicine, University of California Los Angeles, Los Angeles, CA, USA;4. College of Pharmacy and Health Sciences, St. John’s University, Queens, NY, USA
Abstract:Introduction: Current therapeutic approaches for pulmonary arterial hypertension (PAH) commonly include use of prostacyclins, endothelin pathway antagonists or NO (nitric oxide) pathway modulators. These agents are non-specific and suffer from several important shortcomings including short half-lives, invasive routes of administration, higher dose and frequency requirements, and several dose-related systemic side effects. Hence, discovery of novel agents with improved therapeutic efficacy with respect to survival benefits and the development of non-invasive routes of administration are in critical need. Current research aimed at developing more selective therapies for PAH are focused both on agents acting on novel molecular targets, as well as, novel compounds acting on conventional pathways with improved characteristics.

Area covered: The present review covers recently filed (issued/application) patents (2010–2016) describing novel agents acting on investigational targets as well as novel compounds with improved characteristics acting on established targets. Patents describing combinations of conventional and investigational compounds are also discussed.

Expert opinion: PAH has recently been considered as cancer-like disease with over-proliferation of pulmonary arterial smooth muscle cells and endothelial cells. New cellular and molecular biological advances have revealed novel target/pathways involved in the pathogenesis and progression of PAH. Thus, discovery of agents that act on these novel pathways provides a promising avenue of research for improving therapeutic approaches for PAH.

Keywords:Pulmonary hypertension  pulmonary arterial hypertension  novel targets  Rho-kinase inhibitors  tyrosine kinase inhibitors  serotonin uptake inhibitors
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