TABLE 1.

Macrophages targeting therapies in cancers.

Substance	Target	Mechanisms	Tumor type / study type	Side effects	References
Nivolumab	PD1	Enhancing cytotoxic activity and phagocytosis to tumor cells	Glioma:Phase 3	Hypertension, fatigue	Reardon et al., 2020
WP1066	STAT3	Inducing costimulatory molecules expression and increasing immune-stimulatory cytokines production and T-cell proliferation	Glioma:preclinical trial melanoma:Phase 1	Unknown	Hussain et al., 2007
Anti-CD47 antibody	CD47	Enhancing cytotoxic activity and phagocytosis to tumor cells	Glioma:preclinical trial	Unknown	Hayat et al., 2020
OLA-PEG, NOX-A12	SDF-1	Inhibiting the recruitment of TAMs	Glioma:preclinical trial	Unknown	Deng et al., 2017
POL5551	CXCR4	Inhibiting hypoxia-induced glioma cell migration and reducing tumor-initiating GSCs and MGCs populations	Glioma:preclinical trial	Unknown	Gagner et al., 2017
ACF	TGF-α	Blocking hypoxia-induced POSTN over-expression by TGF-α through the RTK/PI3K pathway to inhibit the recruitment of macrophages.	Glioma:preclinical trial	Unknown	Guo et al., 2016
BLZ945	CSF1R	Inhibitor of CSF1R, preventing glioma progression	Glioma:preclinical trial	Unknown	Pyonteck et al., 2013
GK921	TGM2	Triggering MES transdifferentiation of GSCs	Glioma:preclinical trial	Unknown	Yin et al., 2016
STX-0119	STAT3	The STAT3 inhibitor, promoting TILs accumulation	Glioma:preclinical trial	Unknown	Akiyama et al., 2017
FLA-16	CYP4A	Inhibiting angiogenesis	Glioma:preclinical trial	Unknown	Wang et al., 2017
ISL	Akt- FGF-2/TGF-β/VEGF	Inhibiting angiogenesis	Glioma:preclinical trial	Unknown	Wang et al., 2019
Flavonoid CH625	CYP4X1	Inhibiting angiogenesis	Glioma:preclinical trial	Unknown	Wang C. et al., 2018
TrLp	p53	Increasing the TAMs-depletion capability	Glioma:preclinical trial	Unknown	Mukherjee et al., 2018
miR-124	STAT3	Inhibiting the STAT3 pathway and reversing T-cell proliferation immunosuppression	Glioma:preclinical trial	Unknown	Wei et al., 2013
Trabectedin	CCL2-CCR2 axis; caspase-8	Inhibition of macrophage differentiation and cytokine production and improvement of the TAMs-depletion capability	Metastatic soft-tissue sarcomas:Phase 1/2 Breast cancer:Phase 2	Neutropenia, hepatic (transaminitis), fatigue, nausea, vomiting, constipation	Martin-Broto et al., 2020
PLX3397	CSF1R	Inducing gene expression of M2-like macrophages	Tenosynovial giant-cell tumors:Phase 1/2	Changes in hair color, fatigue, nausea, dysgeusia, periorbital edema, diarrhea, hyponatremia, etc.	Tap et al., 2015
AZD1480	ICAM-1 and pSTAT3	Suppressing macrophage infiltration into the tumor site	Lung cancer:Phase I	Dizziness, ataxia, hallucinations, and anxiety	Piao et al., 2017
Ablation of NRP-1	NRP-1	Inhibition of Angiogenesis and interfering the interaction of TAMs with the TME	Breast cancer:preclinical trial	Unknown	Kawaguchi et al., 2017
TMP195	CSF1 and CSF2	Regulating the polarization of TAMs	Breast cancer:preclinical trial	Unknown	Guerriero et al., 2017
Leg-3	Legumain	Activating the ablation of TAMs	Breast cancer:preclinical trial	Unknown	Lin et al., 2013
BLIMP1	CCL8	Suppressing CCL8 expression to modulate host defenses	L. monocytogenes infection:preclinical trial	Unknown	Severa et al., 2014