Aleplasinin

Aleplasinin is a small molecule inhibitor that selectively and potently targets plasminogen activator inhibitor-1 (PAI-1; also known as SERPINE1), a key negative regulator of the fibrinolytic system[1][4][5]. It is orally active and can cross the blood-brain barrier[1]. Aleplasinin was originally developed for Alzheimer's disease research due to its ability to increase amyloid-beta catabolism and ameliorate amyloid-related pathology by inhibiting PAI-1, which enhances plasminogen activation and may promote clearance of amyloid-beta peptides[3][4]. Preclinical studies have shown it improves memory deficiency in models of Alzheimer's disease[1]. The drug was initially developed by Wyeth (later acquired by Pfizer) but its development for Alzheimer's disease has been discontinued after reaching early clinical phases[3][4]. More recently, research suggests potential repurposing in oncology as an inhibitor of Siglec-15 implicated in colorectal cancer progression, with evidence for cytotoxicity against cancer cells and modulation of lipid metabolism pathways[6].

Other names

aleplasininPAZ-417PAZ417PAZ 417