Thursday, October 25, 2012
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BCR-ABL tyrosine kinase
Cell culture studies
suggest Bosulif bosutinib plus danusertib could help treat
CML resistant to Gleevec imatinib. In
primary cancer cells isolated from a patient with Gleevec-resistant CML,
bosutinib and danusertib synergistically decreased cell proliferation
compared with vehicle. The combination did not show a synergistic
antiproliferative effect in cells from a patient with Gleevec-sensitive CML.
Next steps could include testing the combination in a mouse model of
Novartis AG markets the
BCR-ABL inhibitor Gleevec to treat CML and gastrointestinal stromal tumors
Pfizer Inc.'s Bosulif,
a dual inhibitor of BCR-ABL and Src, is approved to treat
Nerviano Medical Sciences s.r.l.'s
kinase inhibitor, danusertib (PHA-739358), is in Phase I
and Phase II testing to treat various cancers.
Published online Oct. 25, 2012
Patent and licensing status
Winter, G.E. et al. Nat.
Chem. Biol.; published online Sept. 30, 2012;
Contact: Giulio Superti-Furga, Research Center for Molecular
Medicine of the Austrian Academy of Sciences, Vienna, Austria
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