Anti-cancer Compounds with Improved Cardiac Safety and Drug Resistance Profiles

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Tyrosine kinase inhibitors are effective targeted anti-cancer therapeutics, but currently available inhibitors have limitations due to drug resistance and cardiotoxic effects. Oregon Health & Science University researchers have developed a class of kinase inhibitors with an improved cardiovascular safety profile and the potential to overcome drug resistance.

Technology Overview

Chronic myeloid leukemia (CML) and acute lymphoblastic leukemia are both associated with the oncogene BCR-ABL, and tyrosine kinase inhibitors targeting this oncogene are first-line treatments for these cancers. However, current TKIs have adverse cardiovascular effects and many patients demonstrate drug resistance. The laboratory of Dr. Sanjay Malhotra has taken a structurally-guided approach to design a novel class of TKI inhibitors with the following properties:

•       Highly potent anti-tumor activity, with IC50s in the low nanomolar range

•       Effective against wildtype BCR-ABL and the T351I mutant that confers drug resistance

•       Improved cardiovascular safety profile up to 10 µM, as determined by iPSC-cardiomyocyte (iPSC-CM) screening

•       Comparable efficacies to ponatinib and durable tumor regression in the K-562 xenograft model in mice with oral administration.

Licensing Opportunity

This technology is available for licensing.


Patent Information:
For Information, Contact:
Anne Carlson
Assoc Dir, Tech Dev & Licensing
Oregon Health & Science University
Sanjay Malhotra
Mallesh Pandrala
Dhanir Tailor
Mark Mercola
Arne Antoon Bruyneel
Therapeutics - Cancer
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