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June 7, 2007
Kinex Pharmaceuticals Presents Recent Data on KXO1 at International Conference
Dr. David Hangauer, Senior VP of Research and Development delivered a case study that described the discovery of KXO1, the Company's clinical drug candidate for oncology. The conference, "Protein Kinase Targets: Drug Discovery and Design", was held in Boston on June 4-6, 2007 and attended by leaders in the field of structure-based drug design and kinase drug development.
Dr. Hangauer's talk was entitled "The Discovery of KXO1: A Highly Selective, Non-ATP Competitive, Src Inhibitor". The presentation centered around Kinex Pharmaceuticals platform technology, MimeticaTM, and its application in generating novel selective molecules like KXO1. KXO1 was discovered as a novel small molecule Src tyrosine kinase inhibitor that targets the peptide substrate binding site rather than the ATP site wherein most tyrosine kinase inhibitors bind. This unique binding site provides much higher selectivity than is obtained with ATP competitive Src inhibitors. KXO1 inhibits Src kinase activity in whole cells with low nM potency and is >1,000-fold less active against other tyrosine kinases such as EGFRTK, PDGFRTK, JAK1, JAK2, ZAP70 and Lck. KXO1 is also a low nM potency inhibitor of tumor cell growth for a broad range of cancer types in vitro and is orally effective in animal tumor models.
KXO1 is currently completing late preclinical development for oncology applications and is expected to enter Phase I clinical trials in 2007.