Drug intelligence / Profile preview

xl999

Development stage
Phase 2
Lead developer
Exelixis
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding 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

PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRA (Platelet-derived growth factor receptor alpha)FGFR3 (Fibroblast growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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