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TT-01488 is a novel, orally bioavailable, non-covalent and reversible small molecule inhibitor of Bruton's tyrosine kinase (BTK). It is designed to overcome acquired resistance to currently marketed covalent BTK inhibitors, particularly those associated with the C481S mutation in BTK. By inhibiting both wildtype and C481S-mutant BTK, TT-01488 disrupts B-cell receptor signaling pathways that are critical for the proliferation and survival of malignant B cells. Preclinical studies have demonstrated potent antitumor activity in B-cell lymphoma models. The drug is being developed primarily for relapsed or refractory B-cell malignancies including various subtypes of non-Hodgkin lymphoma (NHL), chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), Waldenström macroglobulinemia (WM), follicular lymphoma (FL), marginal zone lymphoma (MZL), diffuse large B-cell lymphoma (DLBCL) and other B-cell lymphomas. Phase 1 clinical trials have shown that TT-01488 is well-tolerated with no dose-limiting toxicities observed so far[2][3][4][5].
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