DPT0416

DPT0416 is a novel, CNS-penetrant small molecule inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), being developed primarily for the treatment of Alzheimer's disease. It was initially developed by DP Technology. Lp-PLA2 is an enzyme secreted largely by inflammatory cells (such as macrophages and microglia) and is involved in the hydrolysis of oxidized phospholipids on low-density lipoprotein particles, yielding the inflammatory mediator lysophosphatidylcholine (lysoPC) and other proinflammatory factors. These mediators can produce vascular endothelial injury, increased blood-brain barrier (BBB) permeability, and brain inflammation—all important features of Alzheimer's disease pathogenesis. By inhibiting Lp-PLA2, DPT0416 is intended to improve BBB integrity and reduce neuroinflammation. In animal models, DPT0416 demonstrated improvements in BBB function and reductions in brain inflammatory markers. Compared with prior Lp-PLA2 inhibitors such as Rilapladib, DPT0416 shows higher potency and improved drug-like properties. As of July 2024, DPT0416 is in preclinical development, with IND-enabling studies ongoing for Alzheimer's disease[1][3][5][7].

Other names

DPT0416DPT-0416DPT 0416