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ASKC852 is an orally bioavailable, potent, and highly selective small molecule inhibitor of the transforming growth factor-beta receptor type 1 (TGF-βRI, also known as ALK5). Developed by Aosaikang in collaboration with WuXi AppTec, ASKC852 blocks the TGF-β/SMAD signaling pathway, thereby inhibiting downstream SMAD phosphorylation, tumor epithelial-mesenchymal transition (EMT), metastasis, and angiogenesis, while enhancing the anti-tumor immune response in the tumor microenvironment. Preclinical studies have demonstrated that ASKC852 exhibits significant single-agent anti-tumor activity and synergistic efficacy when combined with anti-PD-L1 antibodies. ASKC852 is currently in Phase I clinical development for the treatment of advanced solid tumors, including breast cancer and liver cancer.
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