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Docirbrutinib is a highly selective, orally bioavailable, non-covalent inhibitor of Bruton's tyrosine kinase (BTK), developed for the treatment of chronic lymphocytic leukemia (CLL) and other B-cell malignancies. Unlike covalent BTK inhibitors such as ibrutinib, docirbrutinib is active against both wild-type and multiple resistant BTK mutations (including C481S, T474x, T316x, L528x), making it a pan-mutant BTK inhibitor. It has demonstrated significant antitumor activity in preclinical models and shows strong synergy with Bcl-2 inhibitors. Docirbrutinib is currently being evaluated in an open-label Phase 1b clinical trial for patients with relapsed or refractory CLL/small lymphocytic lymphoma (SLL) and B-cell non-Hodgkin lymphoma who have failed or are intolerant to at least two lines of systemic therapy[1][2][4][5][7].
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