delcasertib

Delcasertib is a synthetic peptide drug that acts as a selective inhibitor of delta-protein kinase C (PKCδ). It is composed of two main parts: a cargo peptide derived from the δV1-1 region of PKCδ, which inhibits PKCδ translocation, and a cell-penetrating carrier peptide based on the HIV TAT protein sequence to facilitate cellular uptake[1][4]. Delcasertib was developed primarily for the prevention of myocardial tissue death and associated heart failure in patients with acute myocardial infarction undergoing revascularization procedures. The drug works by disrupting the binding of PKCδ to its receptor for activated C kinase, thereby preventing localization to mitochondria during periods of ischemia and reperfusion. This mechanism was shown in preclinical studies to reduce infarct size, enhance recovery of left ventricular function, and improve microvascular patency following acute myocardial infarction[3][6]. Despite promising early results, clinical trials failed to demonstrate significant benefit in reducing cardiac injury biomarkers or improving clinical outcomes when used as an adjunct during percutaneous coronary intervention (PCI) for ST-elevation myocardial infarction (STEMI), leading to discontinuation of further development[4][6].

Other names

delcasertib