Aptose Biosicences & CrystalGenomics Announce Issuance of US Patent

Aptose Biosciences Inc. recently announced that the United States Patent and Trademark Office has issued US Patent No. 9,758,508 titled 2,3-DIHYDRO-ISOINDOLE-1-ON DERIVATIVE AS BTK KINASE SUPPRESSANT, AND PHARMACEUTICAL COMPOSITION INCLUDING SAME. The patent claims numerous compounds, including the CG’806 compound, pharmaceutical compositions comprising the CG’806 compound, and methods of treating various diseases. The patent is expected to provide protection until the end of 2033.

“This newly issued patent represents a major step in protecting the unique structural properties and potentially broad applications of CG’806,” said Dr. William G. Rice, Chairman, President, and Chief Executive Officer of Aptose. “In addition to being developed as an orally bioavailable first-in-class multi-targeted pan-FLT3/BTK inhibitor, it has been shown to impact other relevant oncogenic targets. We look forward to bolstering the patent portfolio through additional findings and applications.”

“Following the execution of the License Agreement, our two organizations have become close allies to ensure the expeditious development of CG’806, and we look forward to continuous progress towards the upcoming IND application,” stated Joong Myung Cho, PhD, Chairman and Chief Executive Officer of CrystalGenomics.

CG‘806 is an oral, first-in-class pan-FLT3/pan-BTK multi-kinase inhibitor. This small molecule demonstrates potent inhibition of wild type and mutant forms of FLT3 (including internal tandem duplication, or ITD, and mutations of the receptor tyrosine kinase domain and gatekeeper region), eliminates AML tumors in the absence of toxicity in murine xenograft models, and represents a potential best-in-class therapeutic for patients with FLT3-driven AML. Likewise, CG’806 demonstrates potent, non-covalent inhibition of the wild type and Cys481Ser mutant of the BTK enzyme, as well as other oncogenic kinases operative in B cell malignancies, suggesting CG’806 may be developed for various B cell malignancy patients (including CLL, MCL, DLBCL and others) that are resistant/refractory/intolerant to covalent BTK inhibitors. CG’806 is currently in pre-clinical development in partnership with CrystalGenomics.

As previously announced on June 8, 2016, Aptose and CrystalGenomics, Inc. entered into an exclusive global option and license agreement focused on the development of CG026806 (CG’806). Aptose is currently undertaking Investigational New Drug (IND) enabling studies and expects to exercise its option to develop and commercialize CG’806 under the agreement and initiate a phase 1 clinical trial by mid 2018. The potential option exercise would occur prior to submission of an IND application in the U.S and, upon exercise, Aptose would have to pay US $2.0 million in cash or in a combination of cash and common shares. Upon exercise of the option, Aptose would own global rights to develop and commercialize the program outside of Korea and China.

CrystalGenomics, Inc. is a commercial stage biopharmaceutical company focused in the structure-based drug discovery and development of novel therapeutics in unmet medical need areas of inflammation, oncology, and infectious disease. In addition to several drug programs in the R&D pipeline, the company has a drug on the market for osteoarthritis and has recently added commercial manufacturing, sales and marketing capabilities through acquisitions. For more information, please visit: www.cgxinc.com or www.crystalgenomics.com. CrystalGenomics, Inc. is listed on KOSDAQ (083790).

Aptose Biosciences is a clinical-stage biotechnology company committed to developing personalized therapies addressing unmet medical needs in oncology. Aptose is advancing new therapeutics focused on novel cellular targets on the leading edge of cancer. The Company’s small molecule cancer therapeutics pipeline includes products designed to provide single agent efficacy and to enhance the efficacy of other anti-cancer therapies and regimens without overlapping toxicities. For further information, please visit www.aptose.com.