Drug intelligence / Profile preview

PST3093

Development stage
Preclinical
Lead developer
Windtree Therapeutics
Modality
Small Molecules
Administration
Intravenous
01

Overview

PST3093 is a small molecule selective activator of the sarcoplasmic reticulum Ca2+ ATPase (SERCA2a), currently in preclinical development by Windtree Therapeutics for the treatment of heart failure, specifically targeting diastolic dysfunction. As the primary metabolite of istaroxime, PST3093 retains the SERCA2a activating properties of its parent compound but lacks the inhibitory effect on the Na+/K+ ATPase pump, potentially offering a more favorable therapeutic profile. It possesses a significantly longer half-life (approximately 9 hours) compared to istaroxime, suggesting potential for chronic administration. Preclinical studies have demonstrated its ability to improve both systolic and diastolic cardiac function (inotropic and lusitropic effects) in models of diabetic cardiomyopathy.

02

Targets

ATP2A2 (Sarco/endoplasmic reticulum calcium ATPase isoform 2a)SERCA2

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