Table 2.

Therapeutic drugs to target microglia.

Drug Name	Target/Function	Suggested Mode of Action	Study Phase	Tumor Types	Identifier	References
PLX3397 (Pexidartinib)	CSF-1R inhibitor	Reduced GAM infiltration	preclinical	GBM	N/A	[112,164]
PLX3397 (Pexidartinib)	CSF-1R inhibitor	GAM elimination	II and I/IIb	rGBM, pGBM	NCT01349036, NCT01790503	[148]
BLZ945	CSF-1R inhibitor	Inhibition of GAM proliferation, blocking of tumor progression, enhancement of CD8+ T cell infiltration	preclinical	GBM	N/A	[97,165]
RG7155 (Emactuzumab)	CSF-1R inhibitor	Alters macrophage polarization and blocks glioma progression	preclinical	GBM	N/A	[97,150]
RG7155 (Emactuzumab)	CSF-1R inhibitor	CSF-R1 inhibition	I	GBM	NCT02323191	[3,149]
Plerixafor (AMD3100)	CXCR4 antagonist	Reduced GAM recruitment by inhibition of chemotaxis	I/II	HGG	NCT01977677, NCT01339039	[144,159,166]
Peptide R	CXCR4 antagonist	M1-like polarization	preclinical	GBM	N/A	[144,145]
MTZ regimen	CCL2 inhibitor	Reduced GAM recruitment by inhibition of chemotaxis	preclinical	GBM	N/A	[161]
WP1066	STAT3 inhibitor	M1-like polarization through STAT3 blocking	I	GBM, glioma	NCT01904123	[137,138,163]

CCL2 = CC chemokine ligand 2; CSF-1R = colony-stimulating factor 1 receptor; CXCR4 = CXC motif chemokine receptor 4 (=SDF-1); GAM = glioma-associated microglia/macrophages; GBM = glioblastoma; HGG = high-grade glioma; MTZ regimen = trimodal non-cytotoxic drugs (minocycline (M), Telmisartan (T), Zoledronic (Z)); pGBM = primary glioblastoma; rGBM = recurrent glioblastoma; STAT3 = signal transducer and activator of transcription 3.