PH-427-PNP

PH-427-PNP is a nanoparticle formulation of PH-427, a small molecule inhibitor targeting the pleckstrin homology (PH) domains of AKT (protein kinase B) and PDK1 (phosphoinositide-dependent kinase-1). By binding to these PH domains, PH-427 prevents the kinases from binding to phosphatidylinositol-3,4,5-trisphosphate (PIP3) at the plasma membrane, thereby inhibiting their activation and the downstream PI3K/AKT signaling pathway. The "PNP" designation refers to its encapsulation within poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles, which improves the delivery and potency of the compound compared to the free drug. This formulation provides sustained release (approximately 90% over 30 days) and has demonstrated significant efficacy in reducing tumor growth and metastasis in orthotopic pancreatic cancer models, particularly in KRAS-mutant cell lines where the free drug was less effective.

Other names

PH-427 PLGA nanoparticlesPH427 PLGA nanoparticlesPH 427 PLGA nanoparticles