Thursday, September 20, 2012
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Mutations in the
extracellular domain of HER2
as markers of susceptibility to ErbB2 inhibitors
In vitro studies identified oncogenic mutations in the ErbB2
extracellular domain and suggest ErbB2 inhibitors could help treat cancers
that harbor such mutations. In human fibroblasts, expression of an ErbB2
gene with an extracellular domain mutation initially identified in lung
adenocarcinoma induced anchorage-dependent proliferation. In murine bone
marrow cells, expression of the mutant ErbB2 rendered cells more
sensitive to ErbB2 inhibitors, including neratinib
compared with expression of wild-type ErbB2 or ErbB2 with
activating mutations in the kinase domain. Next steps include testing ErbB2
inhibitors in clinical trials.
Inc. and Puma
Biotechnology Inc. have neratinib in clinical and
preclinical testing to treat various cancers.
Ingelheim GmbH has Tomtovok
afatinib in clinical testing to treat multiple cancers.
At least nine other companies have ErbB2 inhibitors in development stages
ranging from preclinical to marketed to treat various cancers.
Published online Sept. 20, 2012
unavailable for licensing
Greulich, H. et al.
Proc. Natl. Acad. Sci. USA; published online
Aug. 20, 2012;
Contact: Heidi Greulich,
Broad Institute of MIT and Harvard, Cambridge, Mass.
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