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Lisaftoclax is a novel, orally bioavailable, selective, and potent small molecule inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (Bcl-2). By binding to and inhibiting Bcl-2, lisaftoclax restores apoptotic processes in tumor cells, leading to pro-apoptotic and antineoplastic effects. Overexpression of Bcl-2 is associated with increased drug resistance and tumor cell survival in many cancers. Lisaftoclax has demonstrated strong antitumor activity in hematologic malignancies such as chronic lymphocytic leukemia (CLL), acute myeloid leukemia (AML), myelodysplastic syndromes (MDS), T-cell prolymphocytic leukemia, multiple myeloma, Waldenstrom's macroglobulinemia, breast cancer, solid tumors, systemic lupus erythematosus (SLE), chronic myeloid leukemia (CML), neuroblastoma, gastrointestinal stromal tumors (GIST), and non-small cell lung cancer. The drug is being developed by Ascentage Pharma and has received orphan drug status for several rare hematologic cancers[1][3][4][5][6][7][8].
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