Auspex Pharmaceuticals Receives U.S. Patent on Novel JAK Inhibitor SD-900 Composition-of-Matter Patent Issues Covering SD-900, a Deuterium-Substituted Analogue of Tofacitinib

LA JOLLA, Calif., Nov. 15, 2012 /PRNewswire/ -- Auspex Pharmaceuticals, Inc. today announced that it has been granted U.S. Patent No. 8,299,084 covering the company's novel JAK kinase inhibitor SD-900, a deuterium-substituted analogue of tofacitinib.

"The issuance of a composition-of-matter patent for SD-900 is strong validation of Auspex's technological approach to the creation of important new drugs," said Lawrence C. Fritz, Ph.D., President and Chief Executive Officer of Auspex. "We believe that SD-900 can emerge as an important drug in the JAK inhibitor space, combining the efficacy of tofacitinib with improved metabolic properties." 

The JAK kinases have emerged as important targets for drugs to treat autoimmune diseases including rheumatoid arthritis, inflammatory bowel disease, and psoriasis as well as for the treatment of certain types of cancer. The JAK inhibitor drug tofacitinib was recently approved by the U.S. Food and Drug Administration for the treatment of rheumatoid arthritis and is also in clinical development for additional autoimmune diseases. Auspex believes that SD-900 will retain precisely the intrinsic pharmacological activity of tofacitinib but improve its pharmacokinetics. These properties may allow SD-900 to provide the efficacy of tofacitinib but at a reduced dose, and may also promote the development of a once-a-day JAK inhibitor for use in treating autoimmune diseases.

Auspex's lead compound, SD-809, also incorporates deuterium into its structure and is entering phase 3 clinical trials for the treatment of hyperkinetic movement disorders, specifically, the chorea associated with Huntington's disease.

About SD-900

SD-900 is a novel "JAK inhibitor", a small molecule inhibitor of the Janus Kinase enzyme family.  It is a specific deuterium-substituted analogue of tofacitinib. Deuterium is a safe, naturally occurring, non-radioactive form of hydrogen. Because the substitution of deuterium for hydrogen does not change the shape of a molecule or its electronic structure, it does not change the binding properties of a drug. However, in certain cases these substitutions can have a beneficial effect on increasing the half-life of the drug. Because of these properties of deuterium, Auspex believes that SD-900 will have equivalent efficacy to tofacitinib but with the prospect of improved pharmaceutical properties.

About Auspex Pharmaceuticals

Auspex Pharmaceuticals is a privately held biopharmaceutical company located in La Jolla, California.  The company is a pioneer in the use of deuterium in medicinal chemistry, and its most advanced program is focused on the treatment of hyperkinetic movement disorders including Huntington's disease, Tourette syndrome and tardive dyskinesia.  Its lead compound, SD-809, is a novel inhibitor of the vesicular monoamine transporter 2 (VMAT-2). This drug offers the potential for significant advantages over existing therapies including improved safety, reduced drug-drug interactions, and less frequent dosing. SD-809 is expected to enter phase 3 clinical testing in 2013. Auspex is also exploiting its deuterium chemistry approach to optimize drugs in several additional therapeutic areas. Included in the Auspex portfolio are SD-900, a JAK kinase inhibitor for the treatment of autoimmune diseases, SD-560 for the treatment of fibrotic diseases, as well as other compounds. For more information on Auspex, please visit the company's web site at http://www.auspexpharma.com.

SOURCE Auspex Pharmaceuticals



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