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Lacutoclax + Rocbrutinib is an oral combination therapy consisting of the selective B-cell lymphoma 2 (Bcl-2) inhibitor lacutoclax (LP-108) and the fourth-generation Bruton's tyrosine kinase (BTK) inhibitor rocbrutinib (LP-168). Developed by Guangzhou Lupeng Pharmaceutical, this combination is designed to treat mature B-cell malignancies by dual inhibition of survival and signaling pathways. Rocbrutinib is a novel BTK inhibitor that maintains activity against resistance mutations (such as C481S, T474X, and L528W) by utilizing both covalent and non-covalent binding modes. Lacutoclax selectively targets Bcl-2, an anti-apoptotic protein frequently overexpressed in B-cell cancers. The combination is currently being evaluated in Phase Ib/II clinical trials for patients with mantle cell lymphoma, chronic lymphocytic leukemia, and other B-cell malignancies. Individually, rocbrutinib has received Breakthrough Therapy Designation in China for relapsed/refractory non-GCB DLBCL and is under priority review for relapsed/refractory MCL.
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