Table 2.

Therapies targeting cholesterol metabolism and their effects on the immune tumor microenvironment.

	Drug	Target	Dosage	Effects on the immune tumor microenvironment	References
Targeting cholesterol biosynthesis	Statins	HMGCR	µM doses	Suppresses PD-L1 expression and thus activates the antitumor response.	(54, 99)
	Fatostatin	SREBPs	mg/kg	Decreases Tregs and alleviates CD8+ T cell exhaustion	(100)
	Terbinafine	SQLE	µg/mL	Reduced Tregs in tumors and increase cytotoxic T infiltration.	(101)
Targeting cholesterol esterification	Avasimibe	SOAT1	µM doses	Improves the formation of immune synapses.	(102)
Targeting LXR signalling	RGX-104	LXR	mg/kg	Causes MDSC depletion and increased T cell activation	(103)
Targeting cholesterol transport	Anti-PCSK9 antibodies	PCSK9	µg	Increases the levels of MHC I and MHC II in cells and, therefore, the antitumor activity of lymphocytes.	(104, 105)
Targeting lipid rafts	HP-β-CD	Lipid rafts	mM doses	Enhanced T cell infiltration and alleviated CD8+ T cell exhaustion	(92)
Targeting bile acids	Cholestyramine	Cholic acid Deoxycholic acid	8 mg/day	Reverses the polarization of the TAMs to M2 phenotype.	(106)