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A Novel Class of Molecules for the Treatment of Human Cancers Exhibiting Excessive ErbB-2/HER2 Signalling
Yeda R&D Co. Ltd Israel flag Israel
Abstract ID: 1633
The ErbB family consists of four structurally related receptor tyrosine kinases. Excessive ErbB signalling is associated with enhanced tumorogenesis, and as such serves as a major therapeutic target...
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Introduction/Background

The ErbB family consists of four structurally related receptor tyrosine kinases. Excessive ErbB signalling is associated with enhanced tumorogenesis, and as such serves as a major therapeutic target in a wide array of solid tumour cancers. A member of this family, the human epidermal growth factor receptor 2 (ErbB-2/HER2), is overexpressed in a variety of human cancers, including breast and gastric tumours. ErbB-2/HER2 amplification correlates with elevated metastatic activity and poor prognosis.

Aims/Hypothesis

An innovative and highly potent approach for cancer treatment is proposed here, based on delivering novel nucleic acid-based entities called aptamers targeting ErbB-2/HER2.

Results

Aptamers are single-stranded oligonucleotides that fold into defined architectures and avidly bind to targets such as proteins, with the same effectiveness and affinity associated with mAbs. Using a novel screening technology the research team has identified a multimeric aptamer with pronounced ErbB-2/HER2 inhibitory activity. Preliminary preclinical experiments show that treatment of gastric tumour-bearing mice with trimeric aptamer resulted in reduced tumour growth that was nearly twofold stronger than that achieved with a monoclonal anti-ErbB-2/HER2 antibody.

Conclusion

Remarkably, the antitumor effect exerted by the multimeric anti-ErbB-2/HER2 aptamers is twofold stronger than that elicited by currently available antiErbB-2 monocolonal antibodies.

Relevance/Opportunity

Please enquire quoting reference no. 1633 regarding licensing or codevelopment partnerships.
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FEATURED
Last Updated May 2015
Technology Type THERAPEUTIC
Phase of Development PRECLINICAL
CORPORATION