luxeptinib

Luxeptinib is an orally bioavailable, reversible, non-covalent small molecule inhibitor that targets both FMS-like tyrosine kinase 3 (FLT3) and Bruton's tyrosine kinase (BTK), including wild-type and clinically relevant mutant forms of these kinases. It inhibits FLT3-mediated and B-cell antigen receptor-mediated signaling, resulting in the suppression of proliferation in tumor cells overexpressing FLT3 or BTK. Luxeptinib also inhibits other oncogenic kinases such as MET proto-oncogene receptor tyrosine kinase, RET proto-oncogene receptor tyrosine kinase, discoidin domain-containing receptor 2 (DDR2), Aurora kinase A, and interleukin-2-inducible T-cell kinase (ITK). In addition to its antineoplastic activity in hematologic malignancies like acute myeloid leukemia (AML) and B-cell tumors, luxeptinib has demonstrated inhibition of the NLRP3 inflammasome pathway and inflammatory cytokines IL-1β, IL-6, and TNFα in preclinical models. The drug is being developed by Aptose Biosciences for use primarily in AML, myelodysplastic syndromes/myeloproliferative neoplasms (MDS/MPN), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL), and other B-cell malignancies[1][3][4][5][6][7].

Other names

luxeptinib [USAN]