November 5, 2021

Exploiting LY3009120 and Asciminib Combination to Target TKI-Resistant CML.

In collaboration with Dr. Michael Deininger's group at the Huntsman Cancer Institute (University of Utah), we discovered structurally novel inhibitors of drug-resistant BCR-ABL1 mutants, such as T315I.

One of these structurally novel compounds, LY3009120 is a non-toxic BCR-ABL1 ligand capable of re-sensitizing the myristoyl-binding pocket at clinically tolerable concentrations. Using LY3009120 can be an effective clinical strategy to target BCR-ABL1 mutations that cause resistance to tyrosine-kinase inhibitors.

Link to ASH