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Selective FGFR2 inhibitor
FGFRs are a typical class of receptor tyrosine kinases (RTKs), including four receptors in the family: FGFR1, FGFR2, FGFR3, and FGFR4. They all consist of three parts: an extracellular region, a transmembrane region, and an intracellular tyrosine kinase domain. Abnormal activation of FGFR signaling pathways due to high expression or mutations is closely associated with the occurrence and development of various diseases, including lung cancer, gastric cancer, breast cancer, colorectal cancer, chronic myeloid leukemia, cholangiocarcinoma, glioblastoma, chondrosarcoma, lipomatosis, and bladder cancer. Although multiple multitarget tyrosine kinase inhibitors (TKIs) on the market can be used to treat tumors with FGFR mutations, FGFR is not their primary target. Currently, there are few marketed drugs capable of selectively inhibiting FGFR targets. While the development of FGFR inhibitors brings hope for targeted therapy to patients with FGFR-driven tumors, research on FGFR inhibitors also faces many challenges. These include the development of resistance, dosage limitations due to the toxicity of inhibitor-type drugs, and other key issues that need to be addressed in the future development of FGFR inhibitor drugs.
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