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Mutations in the extracellular domain of HER2 (EGFR2; ErbB2; neu) 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 and afatinib, 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.
Pfizer Inc. and Puma Biotechnology Inc. have neratinib in clinical and preclinical testing to treat various cancers.
Boehringer 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.

SciBX 5(37); doi:10.1038/scibx.2012.994
Published online Sept. 20, 2012

Findings unpatented; 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.