Ajax Therapeutics, Inc., a biopharmaceutical company applying computational chemistry and structure-based technologies to develop novel, selective small molecules for myeloproliferative neoplasms (MPNs), announced the presentation of preclinical data on the company’s next generation Type II JAK2 inhibitor, AJ1-10502, at a poster session held today at the 64th American Society of Hematology (ASH) Annual Meeting and Exposition in New Orleans.
“It’s exciting to see Ajax’s next generation Type II JAK2 inhibitor, AJ1-10502, demonstrate enhanced selectivity and efficacy with a much-improved safety profile than first generation Type II inhibitors”
The poster, entitled “The Second Generation Type II JAK2 inhibitor, AJ1-10502, Demonstrates Enhanced Selectivity, Improved Therapeutic Efficacy and Reduced Mutant Cell Fraction Compared to Type I JAK2 inhibitors in Models of Myeloproliferative Neoplasms (MPNs),” highlights the improved efficacy and disease modifying features of Ajax’s Type II JAK2 inhibitor, AJ1-10502, when compared to the investigational, first generation Type II inhibitor, CHZ868, and the approved market-leading Type I inhibitor, ruxolitinib, in two different mouse models of MPNs.
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In both MPN models studied, AJ1-10502 demonstrated dose dependent improvements in efficacy over ruxolitinib on key blood cell parameters, including reticulocytes and hematocrit, associated with MPNs, as well as superior reductions in spleen weights on par with JAK2 deletion. More importantly, AJ1-10502 caused significant reductions in mutant cell fraction within bone marrow and spleen not observed with ruxolitinib. Distinct from all currently approved JAK2 inhibitors, including ruxolitinib, that bind the Type I conformation of the JAK2 kinase and allow continued JAK/STAT signaling which leads to disease persistence, AJ1-10502 is designed to bind the Type II conformation of the JAK2 kinase. In preclinical studies, investigational Type II JAK2 inhibitors have been shown to overcome disease persistence to ruxolitinib and, most significantly, reduce mutant JAK2 allele burden that drives MPN disease progression. The ASH poster presentation is available on Ajax’s website.
“We’re very encouraged by the first preclinical data on our Type II JAK2 inhibitor program being presented today at the ASH Annual Meeting,” said Craig E. Masse, PhD, Senior Vice President, Discovery Research at Ajax Therapeutics. “Our unique drug discovery capabilities, including state-of-the-art computational and structure-based technologies, have enabled us to develop Type II JAK2 inhibitors, such as AJ1-10502, that target JAK2 with greater precision and potency, while overcoming the limitations of current JAK2 therapies that interact with other JAK-family members and related kinases which limits their efficacy and leads to unwanted side effects.”
SOURCE: Businesswire