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Mesutoclax + orelabrutinib is an all-oral, chemo-free combination regimen being developed by InnoCare for the treatment of various B-cell malignancies. The combination consists of mesutoclax (ICP-248), a novel, highly selective oral B-cell lymphoma 2 (BCL2) inhibitor, and orelabrutinib (ICP-022), an approved selective Bruton's tyrosine kinase (BTK) inhibitor. By targeting both BCL2 and BTK, the regimen simultaneously inhibits two complementary survival pathways in B-cell malignancies to restore apoptosis and block B-cell receptor signaling. The combination is currently in Phase III clinical development for first-line chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) and relapsed/refractory mantle cell lymphoma (MCL), and has received Breakthrough Therapy Designation in China for relapsed/refractory marginal zone lymphoma (MZL).
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