This invention identifies a novel class of ErbB targeting small molecules.
Activation of the ErbB family of tyrosine kinases (EGFR, Her2, Her3) are prevalent in many cancer types and are easily identified in tumor samples. For example, HER2 overexpression is found in 20% of breast cancers, and EGFR mutations are found in 15% of non-small cell lung cancers, consequently, the ErbB family of tyrosine kinases are an attractive target for cancer therapy. Current treatments, such as Herceptin and lapatinib, are limited by negative feedback loops that increase ErbB production and/or activating ligand-induced resistance. The Her2 inhibitor, Lapatinib is less active in the presence of activating ligands for the Her2/Her3 dimer, such as Neuregulin. Here, UCSF researchers describe a family of small molecules that overcome these limitations of existing ErbB-targeting treatments.
This novel invention provides the following advantages:
By developing a screening method specific for activated ErbB complexes in cells, scientists at the University of California, San Francisco and the California Institute for Biomedical Research (CALIBR) have identified a novel class of ErbB inhibitors that selectively target these oncogenic complexes. This treatment has the potential to overcome the limitations of previous generations of ErbB inhibitors.
- Treatment of ErbB-dependent tumors
To develop and commercialize this technology as a clinical therapy.
|United States Of America||Published Application||20190119284||04/25/2019||2016-186|