The Company initiated a first-in-human clinical study of PWT143, a highly selective oral inhibitor of phosphatidylinositide
3-kinase (PI3K) delta, in healthy subjects in June 2015.
Abbreviations: NF-[kappa]B, nuclear factor-kappaB; mapk, mitogen-activated protein kinase; P13K, phosphatidylinositide
3-kinase: Akt, protein kinase B; FAK, focal adhesion kinase; PSG, prostate-specific G-protein-coupled receptor; IL-6, interleukin-6; JNK, c-Jun NH(2)-terminal kinase; TLC, thin layer chromatography; NMR, nuclear magnetic resonance; FBS, fetal bovine serum; DCC, dextran coated charcoal slurry; RT, room temperature; GC-MS, gas chromatography-mass spectrometry; MIC, minimum inhibitory concentration; AIDS, acquired immunodeficiency syndrome; PI, propidium iodide; RI, retention indices; AP-1, activator protein 1; CREB, cAMP response element-binding protein; c/EBP, CCAAT/enhancer binding protein; SAPK, stress-activated protein kinases.
In pre-clinical studies, PWT143 has been found to be a potent and highly selective oral inhibitor of phosphatidylinositide
3-kinase (PI3K) delta, a molecular target that has been shown to play a critical role in the proliferation and survival of hematologic cancer cells.