X-82 Low Toxicity Angiogenesis Inhibitor

Tyrogenex* has developed a novel, patented cancer therapeutic, X-82. The compound, a dual VEGFR/PDGFR inhibitor, is the result of fourteen years of research and development by Dr. Chris Liang, the Tyrogenex Scientific Founder.

X-82 is a small molecule indolinone inhibitor of signaling through the growth factor receptors VEGFR and PDGFR. VEGFR plays a critical role in proliferation of endothelial cells for new vessel formation and PDGFR is important for regulation of pericytes, cells that provide structural and nutrient support for developing vessels. Both receptors are comprised of heterodimers that phosphorylate one another. The phosphorylation event activates the receptors and transduces signals through the Ras and PI3K pathways to promote new protein synthesis and gene expression that result in the morphogenic and cell proliferative properties that control new blood vessel formation.

X-82 was designed to reduce the toxicity while maintaining the efficacy of existing VEGFR/PDGFR inhibitors.  In December of 2010, Xcovery initiated a First-in-human Phase I clinical trial for X-82 in advanced solid tumors.  The trial is being conducted at Sarah Cannon Research Institute under the direction of Dr. Johanna Bendell.

*Tyrogenex is a part of the Xcovery Group of companies, founded by Biocatalyst International.