SAR103168

SAR103168 is a synthetic small molecule, multi-targeted tyrosine kinase inhibitor of the pyrido[2,3-d]pyridimidine subclass. It exhibits potent inhibitory activity against the entire Src kinase family, BCR-Abl kinase, angiogenic receptor kinases including vascular endothelial growth factor receptor 1 and 2 (VEGFR1/2), Tie2, platelet-derived growth factor receptor (PDGFR), fibroblast growth factor receptors 1 and 3 (FGFR1/3), and epidermal growth factor receptor (EGFR). SAR103168 has demonstrated anti-proliferative and pro-apoptotic effects in acute myeloid leukemia (AML) and chronic myeloid leukemia (CML) cell models at nanomolar concentrations. In preclinical studies, it impaired tumor growth in animal models of AML/CML. Clinical development included phase I trials for relapsed/refractory AML and high-risk myelodysplastic syndrome (MDS); however, further development was discontinued due to unpredictable drug exposure[4][5][6][7][8].