PKC Inhibitor AEB071 Demonstrates Pre-Clinical Activity In Chronic Lymphocytic Leukemia
ElGama D, Zhong Y, Williams K et al.
Key Points:
PKC-β important for survival of B-CLL cells in vivo and essential to CLL development in mouse model (TCL1).
a new inhibitor of PKC - sotrastaurin (AEB071) which is an oral PKC inhibitors with a strong specific activities on PKC-α, PKC-β and PKC-θ and some activities on PKC-δ, PKC-ε, and PKC-η.
Authors investigated activity of sotrastaurin against CLL cells.
AEB071 markedly cytotoxic to CLL B-cells with no significant cytoxic effect on T-cells or NK-cells in CLL patient samples.
Implications:
- PKC-β represents new target for CLL therapy and future efforts targeting PKC with the PKC inhibitor AEB071 may be warranted.
View the original abstract on the ASH website.
