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Publication and contact information


Non-small cell lung cancer (NSCLC)

Epidermal growth factor receptor (EGFR)

A high throughput screening study suggests the staurosporine-based research compound Gö6967 could aid the development of new treatments for NSCLCs with resistance mutations in EGFR. In human NSCLC lines, Gö6967 inhibited proliferation of cell lines with resistance mutations in EGFR, including the T790M mutation, at nanomolar IC50 values. In mice with NSCLC tumors that had a resistance mutation in EGFR, the structurally related compound midostaurin reversibly inhibited the mutant protein and decreased tumor growth compared with vehicle. Next steps include determining whether human pharmacokinetic data will support the use of midostaurin in patients with lung cancer that have resistance mutations in EGFR.
Novartis AG's midostaurin, a protein kinase C (PKC) inhibitor, is in Phase III testing to treat acute myelogenous leukemia (AML).

SciBX 6(2); doi:10.1038/scibx.2013.34
Published online Jan. 17, 2013

Patent and licensing status undisclosed

Lee, H.-J. et al. Cancer Discov.; published online Dec. 10, 2012;
Contact: Jeff Settleman, Genentech Inc., South San Francisco, Calif.