Shaw, Duncan, Hollingworth, Gregory, Soldermann, Nicolas, Sprague, Elizabeth, Schuler, Walter, Vangrevelinghe, Eric, Duggan, Nicholas, Thomas, Matthew, Kosaka, Takatoshi, 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