Preferred Label : Vimseltinib;
NCIt synonyms : CSF1R Inhibitor DCC-3014;
NCIt definition : An orally bioavailable inhibitor of the tyrosine kinase receptor colony stimulating
factor 1 receptor (CSF1R; CSF-1R; C-FMS; CD115; M-CSFR), with potential antineoplastic,
macrophage checkpoint-inhibitory and immunomodulating activities. Upon administration,
vimseltinib targets and binds to CSF1R expressed on monocytes, macrophages, and osteoclasts
and inhibits the binding of the CSF1R ligands colony-stimulating factor-1 (CSF-1)
and interleukin-34 (IL-34), to CSF1R. This prevents CSF1R activation and CSF1R-mediated
signaling in these cells. This blocks the production of inflammatory mediators by
macrophages and monocytes and reduces inflammation. By blocking the recruitment to
the tumor microenvironment (TME) and activity of CSF1R-dependent tumor-associated
macrophages (TAMs), vimseltinib inhibits the immunomodulating activity by macrophages
and enhances T-cell infiltration and anti-tumor T-cell immune responses, which inhibits
the proliferation of tumor cells. TAMs play key roles in the TME and allow for immune
suppression; TAMs promote inflammation, tumor cell proliferation, angiogenesis, invasiveness
and survival.;
UNII : PX9FTM69BF;
InChIKey : TVGAHWWPABTBCX-UHFFFAOYSA-N;
CAS number : 1628606-05-2;
Molecule name : DCC-3014; DP-6865; DCC 3014;
NCI Metathesaurus CUI : CL523727;
Origin ID : C175876;
UMLS CUI : C5446811;
Semantic type(s)
chemical_or_drug_has_mechanism_of_action
concept_is_in_subset
has_target