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Orantinib is an orally bioavailable small molecule receptor tyrosine kinase inhibitor that targets multiple kinases involved in tumor angiogenesis and cell proliferation. Specifically, it inhibits the autophosphorylation of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor (PDGFR), fibroblast growth factor receptor (FGFR), and also the stem cell factor receptor c-kit. By blocking these pathways, orantinib suppresses angiogenesis and tumor cell proliferation. Orantinib was originally developed by Sugen (now part of Pfizer) and later co-developed with Taiho Pharmaceutical. It has been investigated primarily for various solid tumors including hepatocellular carcinoma, breast cancer, lung cancer, kidney cancer, gastric cancer, prostate cancer, pancreatic neoplasms, plasma cell neoplasms, and colorectal cancer. The most advanced clinical development reached phase III trials for unresectable hepatocellular carcinoma; however, this program was terminated in 2014 due to lack of efficacy[1][3][4][6].
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