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xl999
- Development stage
- Phase 2
- Lead developer
- Exelixis
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
XL999 is a small molecule multi-targeted tyrosine kinase inhibitor developed as an investigational anticancer agent. It inhibits several receptor tyrosine kinases (RTKs) involved in tumor growth and angiogenesis, including fibroblast growth factor receptors 1 and 3 (FGFR1/3), vascular endothelial growth factor receptor 2 (VEGFR2/KDR), platelet-derived growth factor receptors alpha and beta (PDGFRα/β), KIT, FMS-like tyrosine kinase 3 (FLT3), FLT4, RET, and SRC. By blocking these kinases, XL999 disrupts both tumor cell proliferation directly and the formation of new blood vessels that supply tumors. Preclinical studies demonstrated broad antitumor activity in xenograft models. Clinical development reached phase II for some indications but was discontinued for all known cancer types[1][2][5][8].
- Other names
- Tyrosine kinase-IN-1705946-27-66I7PLF6N8L
02
Targets
FGFR1 (Fibroblast growth factor receptor 1)FGFR3 (Fibroblast growth factor receptor 3)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)RET (Rearranged during transfection receptor tyrosine kinase)SRC (Proto-oncogene tyrosine-protein kinase Src)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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