On April 19, 2017 Aptose Biosciences Inc. (NASDAQ:APTO) (TSX:APS), a clinical-stage company developing highly differentiated therapeutics that target the underlying mechanisms of cancer, reported that preclinical data for its pan-FLT3/BTK inhibitor CG’806 will be presented in two separate posters at the 2017 American Association for Cancer Research (AACR) (Free AACR Whitepaper) Conference Hematologic Malignancies: Translating Discoveries to Novel Therapies, being held May 6-9 in Boston, MA (Press release, Aptose Biosciences, APR 19, 2017, View Source [SID1234518612]).

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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 Knight Cancer Institute at Oregon Health & Science University (OHSU), will present data related to the potency of CG’806 against various hematologic malignancy cell lines and patient bone marrow specimens. In a separate presentation, Aptose scientists, with researchers from the MD Anderson Cancer Center, will present data demonstrating CG’806’s potent activity against AML cells harboring specific wild type or mutant forms of FLT3.

Abstract Details

Title: "CG’806, a first-in-class FLT3/BTK inhibitor, exhibits potent activity against AML patient samples with mutant or wild-type FLT3, as well as other hematologic malignancy subtypes"
Presenter: Stephen E. Kurtz, Ph.D, Oregon Health & Science University, Portland, OR
Date/Time: May 7, 2017 / 1:00 p.m. ET – 3:00 p.m. ET
Location: Harbor 1/2, Westin Boston Waterfront, Boston, MA
Session: Poster Session
Abstract Details

Title: "CG’806, a first-in-class FLT3/BTK inhibitor, exerts superior potency against AML cells harboring ITD, TKD and gatekeeper mutated FLT3 or wild-type FLT3"
Presenter: Weiguo Zhang, M.D., Ph.D, UT MD Anderson Cancer Center, Houston, TX
Date/Time: May 7, 2017 / 1:00 p.m. ET – 3:00 p.m. ET
Location: Harbor 1/2, Westin Boston Waterfront, Boston, MA
Session: Poster Session
About CG’806

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.