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Pelcitoclax is a second-generation small molecule and a dual inhibitor of the anti-apoptotic proteins B-cell lymphoma 2 (Bcl-2) and Bcl-xL. It acts as a BH3 mimetic that selectively binds to and inhibits these pro-survival proteins, restoring apoptotic processes in tumor cells dependent on Bcl-2/Bcl-xL. This mechanism leads to inhibition of cell proliferation in various cancers where these proteins are overexpressed and associated with drug resistance. Pelcitoclax has demonstrated strong pro-apoptotic activity in preclinical models and is being investigated for its antitumor effects both as monotherapy and in combination with chemotherapy agents such as paclitaxel. Developed by Ascentage Pharma, it has shown promising safety profiles and preliminary efficacy signals in early-phase clinical trials for relapsed/refractory small cell lung cancer (SCLC) and other malignancies[1][2][3][4][5][8].
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