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BT-1053 is a potent, highly selective, and irreversible small molecule inhibitor of Bruton's tyrosine kinase (BTK), developed by Chengdu Better Pharmaceutical Co., Ltd. BTK is a critical component of the B-cell receptor (BCR) signaling pathway, which plays a vital role in the survival and proliferation of malignant B cells. By covalently binding to the Cys481 residue in the ATP-binding pocket of BTK, BT-1053 blocks downstream signaling cascades, including PLCγ2 and NF-κB, leading to reduced cell growth and induced apoptosis in malignant B cells. The drug is primarily being investigated for the treatment of various B-cell non-Hodgkin lymphomas, including chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), and Waldenstrom's macroglobulinemia (WM). It is currently undergoing clinical evaluation in Phase 1/2 trials in China.
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