Selective Inhibition of Activated ErbB Tyrosine Kinases

Tech ID: 25957 / UC Case 2016-186-0

Invention Novelty

This invention identifies a novel class of ErbB targeting small molecules.

Value Proposition

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:

  • Selectively inhibits activated ErbB
  • Inhibition is independent of oncogenic mechanism
  • Target is a gene family mutated in many cancers

Technology Description

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.

Application

- Treatment of ErbB-dependent tumors

Looking for Partners

To develop and commercialize this technology as a clinical therapy.

Stage of Development

Preclinical

Data Availability

Under NDA/CDA

Patent Status

Country Type Number Dated Case
United States Of America Published Application 20190119284 04/25/2019 2016-186
 

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Inventors

  • Novotny, Christopher J.
  • Shokat, Kevan M.

Other Information

Keywords

Small Molecules, ErbB Tyrosine Kinases, Inhibitors, Cancer, Therapeutics

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