Thursday, September 5, 2013
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growth factor receptor 1 (EGFR1;
tumor and mouse studies suggest Src inhibitors could help treat brain
metastases from breast cancer. In patients who have HER2+, metastatic breast cancer and
mouse models of HER2+ or triple-negative breast cancer, Src expression and activation
levels were higher in brain metastases than those in the primary tumors. In
mice xenograft models with HER2+ or triple-negative brain
plus a Src inhibitor decreased tumor growth and increased survival compared
with either agent alone. Ongoing work includes confirming the findings in the
mouse models using the Src inhibitor Sprycel
plc markets Tykerb, a HER1 and HER2 kinase inhibitor, to
treat breast cancer.
Squibb Co. and Otsuka
Pharmaceutical Co. Ltd. market Sprycel, a small molecule
inhibitor of BCR-ABL
tyrosine kinase and Src, to treat acute lymphoblastic
leukemia (ALL) and chronic myelogenous leukemia (CML). The partners also have
the drug in Phase II testing to treat breast and pancreatic cancers and Phase
I testing to treat leukemia.
a dual inhibitor of BCR-ABL and Src, is marketed to treat CML and in Phase II
testing to treat polycystic kidney disease (PKD).
Pharmaceuticals LLC and Hanmi
Pharmaceutical Co. Ltd. have KX01
a selective, small molecule, non-ATP Src inhibitor, in Phase II testing or
earlier to treat various cancers.
Published online Sept. 5, 2013
Unpatented; available for
Zhang, S. et al. Cancer
published online Aug. 1, 2013;
Contact: Dihua Yu, The University of Texas MD Anderson
Cancer Center, Houston, Texas
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