cafusetinib

Cafusetinib (SHR1258) is an orally bioavailable, small-molecule tyrosine kinase inhibitor (TKI) that selectively targets the mesenchymal-epithelial transition (MET) receptor, also known as hepatocyte growth factor receptor (HGFR). Developed by Jiangsu Hengrui Medicine, cafusetinib is designed to inhibit the autophosphorylation of MET and its downstream signaling pathways, including PI3K/AKT and MAPK/ERK, which are critical for tumor cell proliferation, survival, and metastasis. Dysregulation of MET signaling, often driven by gene amplification, protein overexpression, or specific mutations such as MET exon 14 skipping, is a significant oncogenic driver in various cancers, particularly non-small cell lung cancer (NSCLC) and gastric cancer. Cafusetinib is currently being evaluated in clinical trials for the treatment of advanced solid tumors that harbor these MET alterations.