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. 2020 Nov 30;28(7):4030–4048. doi: 10.1245/s10434-020-09371-z

Table 3.

Possible and rational therapies targeting MDSCs for pre-metastatic niche disruption after tumor resection

Strategies Drugs Clinical trial Mechanisms Reference
Anti-surgical stress β-blockade (Propranolol) NCT03152786/NCT02013492 Block the β2-AR signal in MDSCs 109
COX-2 inhibitor (Celecoxib, Etodolac) NCT03896113/NCT03864575/NCT03838029 Disruption of the COX-2/PGE-2 signals; reducing MDSC recruitment and differentiation, repressing MDSC-associated suppressive factors such as Arg-1 and ROS production 81
Anti-DAMPs Anti-HMGB 1 antibody Preclinical Ameliorated the trauma-induced attenuated T-cell responses and accumulation of MDSCs in the spleens seen 2 days after injury 44
S100A8/A9 neutralizing antibody Preclinical Neutralizing extracellular S100A8/A9 119
Anti-inflammatory signals NF-κB inhibitor (BAY11-7082) Preclinical Inhibiting NF-κB mediated CXCL1, CXCL2 and CXCL5 production, that reduce the chemotaxis of MDSCs; Inhibition NLRP3 inflammasome activation and the increased pyroptosis 124
NLRP3 inhibitor (MCC950/CY-09/OLT1177/Tranilast/Oridonin) Preclinical Inhibition NLRP3 inflammasome activation and the following IL-1β secretion 121
IL-1β (Anakinra) NCT02780583/NCT04359784 Inhibit the IL-1β inducing CCL5, CXCL12, CCL2, and CXCL5 expression 50
Epigenetic drugs HDAC (Entinostat) NCT01207726/NCT03501381/NCT03552380 Downregulating CCR2 and CXCR2 expression; promoting MDSC differentiation into a more-interstitial macrophage-like phenotype 5
DMNT (5-azacytidine) NCT01207726/NCT03709550
Depletion of MDSCs Chemotherapy (Gemcitabine/5-FU) NCT04331626/NCT01803152/NCT02090101 Depletes G-MDSCs, M-MDSCs, macrophages, and eosinophils 142
TKI(Pazopanib/Bevacizumab) NCT01832259/NCT01218048 Blockade of VEGF and c-KIT signaling; inhibit STAT3 129
Differentiating MDSCs ARTA NCT02403778 Inhibits retinoic signaling to shift the differentiation of MDSC into mature myeloid cells, such as macrophages and dendritic cells 147
Blocking MDSCs trafficking CXCR2 inhibitor (AZD5069, Reparixin, SX-682) NCT03161431/NCT02499328/NCT02370238 Inhibit CXCR2 mediated MDSCs trafficking 94
CCR2 inhibitor (BMS-813160, RS504393) NCT04123379/NCT03767582/NCT03496662 Improved the prognosis by blocking chemotaxis of M-MDSCs 142
Inhibit MDSCs activity Stat3 inhibitor (AZD9150) NCT02499328 A marked decrease in G-MDSC within the peripheral blood mononuclear cells 158
NF-κB inhibitor (BAY11-7082) Pre-clinical Inhibit the activated NF-kB signal induced by DAMPs-PRR interaction 42
Targeting the ECM remodeling LOX inhibitor (β-aminopropionitrile) Pre-clinical Reduce the surgery induced hypoxia related LOX, and ECM remodeling 161
Repair vascular leakage IL-6 inhibitor (Tocilizumab) NCT04370834) Inhibit IL-6 mediated inflammatory response the repair the vascular leakage 164
C5 antibody (Ravulizumab) NCT04369469 Inhibit the C5a-C5R signal on vascular endothelial cells 165
Restore the immunity after surgery TGF-β inhibitor (LY3200882/LY2157299/EW-7197) NCT04031872/NCT03143985/NCT02452008 Reverse the MDSC secreted TGF-β mediated immunosuppression 166
PDE5 inhibitor (Sildenafil, Tadalafil) NCT02544880 Targeting MDSC expression and function of Arg-1 and iNOS 167169
ERAS NCT02644603 Pre-rehabilitation, nutrition, pain management to rapid restore immunity after surgery 172