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Ifebemtinib is an orally bioavailable, highly selective small molecule inhibitor of focal adhesion kinase (FAK), also known as protein tyrosine kinase 2 (PTK2). It acts by competitively inhibiting the ATP-binding site of PTK2, thereby blocking downstream signaling pathways involved in tumor cell migration, proliferation, invasion, and survival. FAK/PTK2 is a cytoplasmic tyrosine kinase that functions as a signal transducer for integrins and is overexpressed in various tumor types. Ifebemtinib has demonstrated significant antineoplastic activity and therapeutic synergy with chemotherapy agents, targeted therapies (notably KRAS inhibitors), and immunotherapies. The drug was originally developed by Boehringer Ingelheim and further advanced by InxMed. It has received Breakthrough Therapy Designation from the China NMPA for first-line treatment of non-small cell lung cancer (NSCLC) with KRAS G12C mutation in combination with garsorasib, as well as for platinum-resistant ovarian cancer in combination with PEG-liposomal doxorubicin. Clinical trials are ongoing or completed in NSCLC (including KRAS G12C-mutant), ovarian cancer, colorectal cancer, melanoma, pancreatic cancer, breast cancer, head and neck cancers, small cell lung cancer, and solid tumors[1][3][4][5][6][8][10].
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