Leads for the treatment of pulmonary hypertension.
BACKGROUND
Knowledge of the causative reasons for pulmonary arterial hypertension, a major category of pulmonary hypertension, has expanded dramatically over the past 10 years. This has led to heightened research across a range of potential new mechanistic approaches and resulted in the identification of further treatment options, together with several promising leads and prototypes.


OBJECTIVE
This review aims to summarise and assess the most relevant research fields, covering key publications and recent patent literature.


METHODS
Searching revealed in excess of 700 patents claiming uses that relate to pulmonary hypertension. These patents were filtered into key therapeutic approaches based on pharmacological reviews of the pulmonary arterial hypertension field.


CONCLUSIONS
Endothelin antagonists and phosphodiesterase 5 inhibitors have emerged as recently approved treatment options and are proving extremely beneficial. Further new mechanistic approaches have yielded promising leads, some of which have the potential to be disease modifying; notably, tyrosine kinase inhibitors, soluble guanylate cyclase agonists, Rho-kinase inhibitors, vasoactive intestinal peptide analogues and 5-HT antagonists.
Palmer
Michael J
MJ
Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent, UK. mike.palmer@pfizer.com
D000818:Animals; D015195:Drug Design; D065128:Endothelin Receptor Antagonists; D020536:Enzyme Activators / Q000494:pharmacology / Q000627:therapeutic use; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D006976:Hypertension, Pulmonary / Q000188:drug therapy* / Q000503:physiopathology; D010330:Patents as Topic; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D011453:Prostaglandins / Q000494:pharmacology / Q000627:therapeutic use
D065128:Endothelin Receptor Antagonists; D020536:Enzyme Activators; D004791:Enzyme Inhibitors; D010726:Phosphodiesterase Inhibitors; D011453:Prostaglandins