Preferred Label : CSF-1R/DDR1/VEGFR2 Inhibitor C019199;
NCIt synonyms : CSF-1R Inhibitor C019199;
NCIt definition : An orally bioavailable inhibitor of colony stimulating factor 1 receptor (CSF1R; CSF-1R;
CD115; M-CSFR), discoid domain receptor type 1 (DDR1) and vascular endothelial growth
factor receptor type 2 (VEGFR2), with potential antineoplastic activity. Upon oral
administration, CSF-1R/DDR1/VEGFR2 inhibitor C019199 targets, binds to and inhibits
the activity of CSF-1R. This inhibits CSF1R activation and CSF1R-mediated signaling,
thereby inhibiting the activities of tumor-associated macrophages (TAMs) and myeloid-derived
suppressor cells (MDSCs), and preventing immune suppression in the tumor microenvironment
(TME). This enhances antitumor T-cell immune responses and inhibits the proliferation
of tumor cells. CSF1R, also known as macrophage colony-stimulating factor receptor
(M-CSFR) and CD115 (cluster of differentiation 115), is a cell-surface receptor that
plays major roles in tumor cell proliferation and metastasis. C019199 also targets,
binds to and inhibits the activity of DDR1 and VEGFR2. Blocking DDR1, a protein expressed
on tumor cells that binds collagen to make a minimally permeable physical barrier
that blocks immune cells in the TME from interacting with and attacking the tumor,
causes the collagen fibers to lose alignment and loosen. This creates gaps in the
tumor barrier, thereby allowing cytotoxic T-cells to enter and attack the tumor. Blocking
VEGFR2 results in the inhibition of tumor angiogenesis and tumor cell proliferation.;
Molecule name : C-019199; C 019199;
NCI Metathesaurus CUI : CL1928607;
Origin ID : C206273;
concept_is_in_subset
- has_target
