Design of Platelet Derived Growth Factor Receptor Inhibitors for Inhalation as a Treatment for Lung Remodeling in Pulmonary Arterial Hypertension: Optimization for Duration of Action
Shaw DE, Baig F, Konstantinova I, Stringer R, Sviridenko L, Tomlins C, Pearce A.
Respiratory Drug Delivery 2018. Volume 1, 2018: 51-60.
Abstract:
A series of potent platelet derived growth factor receptor (PDGFR) inhibitors have been optimized for duration of action in the lung. Examination of pharmacokinetic/pharmacodynamic (PK/PD) data from the optimization effort has revealed in vitro-in vivo correlations which link duration of action in vivo with low permeability and high basicity, and demonstrate that nonspecific binding to lung tissue increases with lipophilicity.
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