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Aptose Biosciences to Present CG’806 Data at AACR Hematologic Malignancies Meeting
Aptose is developing CG’806, a first-in-class pan-FLT3/BTK inhibitor, for acute myeloid leukemia (AML) and other hematologic malignancies. CG’806 is a highly potent inhibitor of the wild type and mutant forms of FLT3 (including internal tandem duplication, or ITD, and mutations of the receptor tyrosine kinase domain and the 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. In addition, CG’806 is a reversible, non-covalent, inhibitor of the wild type and mutant forms of the BTK enzymes. The spectrum of activity against specific clusters of kinase enzymes supports the development of CG’806 for AML, certain B cell malignancies and other hematologic malignancies.
Two separate presentations are planned for CG’806. Aptose scientists, with researchers from the
CG’806 is a once daily, oral, first-in-class pan-FLT3/BTK inhibitor. This small molecule demonstrates potent inhibition of 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 Cys481Ser mutant of the BTK enzyme, as well as other oncogenic kinases operative in B cell malignancies, suggesting the CG’806 may be developed for CLL and MCL patients that are resistant/refractory/intolerant to covalent BTK inhibitors.
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