Bioactive small molecule development- IRAK-FLT3 program

National Center For Advancing Translational Sciences

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Abstract

Acute myeloid leukemia (AML) is a blood cell cancer that is estimated to cause ~100,000 deaths worldwide each year. Current standard of care includes treatment with chemotherapeutic agents, newer targeted therapies such as FLT3 kinase inhibitors, and in some cases, hematopoietic stem cell transplantation. Despite the availability of these treatment options, a diagnosis of AML is, for most patients, a death sentence, with only 32% surviving at least 5 years post-diagnosis. This program involves the discovery of a series of dual IRAK/FLT3 inhibitors with remarkable activity in selected AML models including in resistant AML cell lines carrying point mutations in tyrosine kinase domain (TKD).