Category: Nature Biotechnology
Quizartinib (AC220) in Patients With FLT3-ITD(+) Relapsed or Refractory Acute Myeloid Leukemia: Final Results of a Randomized Phase 2 Study
Background FLT3-ITD in AML is associated with early relapse and poor survival after treatment with standard chemotherapy Quizartinib is an orally active FLT3-ITD inhibitor A previous Phase 2 study included subjects with FLT3-ITD(+) AML, relapsed/refractory to 2nd line chemotherapy or relapsed after hematopoietic stem cell transplant (HSCT), doses of 90, 135 or 200 mg/day – 46% of subjects achieved CRc (CRc = CR + CRp + CRi) – 35% of subjects were bridged to HSCT (mostly after achieving CRi) –…
A small molecule–kinase interaction map for clinical kinase inhibitors
Kinase inhibitors show great promise as a new class of therapeutics. Here we describe an efficient way to determine kinase inhibitor specificity by measuring binding of small molecules to the ATP site of kinases. We have profiled 20 kinase inhibitors, including 16 that are approved drugs or in clinical development, against a panel of 119 protein kinases. We find that specificity varies widely and is not strongly correlated with chemical structure or the identity of the intended target. Many novel…