Drugs /
blz945
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Overview
NCI Definition [1]:
An orally bioavailable inhibitor of colony stimulating factor 1 receptor (CSF-1R; CSF1R), with potential antineoplastic activity. CSF1R inhibitor BLZ945 selectively binds to CSF1R expressed on tumor-associated macrophages (TAMs), blocks the activity of CSF1R, and inhibits CSF1R-mediated signal transduction pathways. This inhibits the activity and proliferation of TAMs, and reprograms the immunosuppressive nature of existing TAMs. Altogether, this reduces TAM-mediated immune suppression in the tumor microenvironment, re-activates the immune system, and improves anti-tumor cell responses mediated by T-cells. CSF1R, also known as macrophage colony-stimulating factor receptor (M-CSFR) and CD115 (cluster of differentiation 115), is a cell-surface receptor for its ligand, colony stimulating factor 1 (CSF1); this receptor is overexpressed by TAMs in the tumor microenvironment, and plays a major role in both immune suppression and the induction of tumor cell proliferation.
Clinical Trials
Blz945 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating blz945, 1 is phase 1/phase 2 (1 open).
Malignant solid tumor is the most common disease being investigated in blz945 clinical trials [2].
Drug Details
Synonyms [2]:
4-[2((1r,2r)-2-hydroxycyclohexylamino)-benzothiazol-6-yloxyl]-pyridine- 2-carboxylic acid methylamide, blz 945, blz-945, 4-((2-(((1r,2r)-2-hydroxycyclohexyl)amino)benzo[d]thiazol-6-yl)oxy)-n-methylpicolinamide, csf-1r inhibitor blz945
Drug Target(s) [2]:
CSF1R
NCIT ID [1]:
C129653
References
1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].
2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.
