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Inflammatory disease

Inducible T cell kinase (ITK)

In vitro and in vivo studies have identified a tetrahydroindazole-based ITK inhibitor called GNE-9822 that could help treat inflammatory disorders. ITK has been linked to various inflammatory conditions including asthma. In vitro, GNE-9822 inhibited ITK with nanomolar potency but affected only 6 of 286 off-target kinases. In mice, rats and dogs, GNE-9822 was orally bioavailable with half-lives of 2.9, 3.0 and 5.4 hours, respectively. Next steps could include evaluating GNE-9822 in animal models of various inflammatory diseases.
Researchers from Roche's Genentech Inc. unit, Evotec AG and Pharmaron Beijing Co. Ltd. contributed to the study. The developmental status of GNE-9822 is unavailable.
Japan Tobacco Inc. has the oral ITK inhibitor JTE-051 in Phase I testing to treat autoimmune diseases and allergies.

SciBX 7(28); doi:10.1038/scibx.2014.832
Published online July 24, 2014

Patent and licensing status unavailable

Burch, J.D. et al. J. Med. Chem.;
published online June 11, 2014;
Contact: Jason D. Burch, Genentech Inc., South San Francisco, Calif.