Inhibition Of PI3K-δ and -γ Isoforms By IPI-145 In Chronic Lymphocytic Leukemia Overcomes Signals From PI3K/AKT/S6 Pathway and Promotes Apoptosis
Balakrishnan K, Peluso M, Fu M, et al.




Key Points:
  • Preclinical data of IPI-145, potent orally bioavailable compound with PI3K-δ and PI3K-γ inhibitory property, reported in this abstract

  • IPI-145 induced significant apoptosis in primary CLL cells, accompanied by decreased expression of anti-apoptotic protein Mcl-1

  • Prognostic markers such as IGHV status, 13q had no impact on sensitivity of CLL cells to compound

  • IPI-145 was as equipotent as ibrutinib and GS-1101 in promoting apoptosis

  • It also demonstrated anti-proliferative and anti-migration effects at nanomolar concentrations

Implications:

  • Data support further development of this agent in B-cell malignancies, including CLL

View the original abstract on the ASH website.






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