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Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension

Shaw, Duncan and Hollingworth, Gregory and Soldermann, Nicolas and Sprague, Elizabeth and Schuler, Walter and Vangrevelinghe, Eric and Duggan, Nicholas and Thomas, Matthew and Kosaka, Takatoshi and Waters, Nigel and Van Eis, Maurice (2014) Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension. Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension, 24 (20). pp. 4812-4817.

Abstract

A novel class of selective inhibitors of ROCK1 and ROCK2 has been identified by structural based drug design. PK/PD experiments using a set of highly selective Rho kinase inhibitors suggest that systemic Rho kinase inhibition is linked to a reversible reduction in lymphocyte counts. These results led to the consideration of topical delivery of these molecules, and to the identification of a lead molecule 7 which shows promising PK and PD in a murine model of pulmonary hypertension after intra-tracheal dosing.

Item Type: Article
Keywords: Rho kinase Inhibitors Lymphocyte depletion Pulmonary arterial hypertension Intra-tracheal dosing
Date Deposited: 13 Oct 2015 13:12
Last Modified: 13 Oct 2015 13:12
URI: https://oak.novartis.com/id/eprint/22342

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