. 2019 Feb 15;11(2):529–541.

Table 1.

Current small molecule inhibitors targeting immune checkpoints and cellular pathways in the tumor microenvironment

Immune checkpoint	Small molecule inhibitors	Cell pathways	References
PD-1/PD-L1	BMS-8, 37, 202, 230, 242, 1001, 1166, SB415286^, vorinostat^, panobinostat^, azacitidine^, decitabine^, entitostat^, JQ1^, I-BET151^, GSK503^*	Invasion	[27,39,40,42,50,77,94]
		Angiogenesis
		T-Cell suppression
		Immunoregulation
CTLA4	Compounds “8 and 9”, entitostat^, panobinostat^, ACY-241^, azacytidine^	Angiogenesis	[42,54,55,95]
		Immune control
		T-Cell activation
		Cell signaling
OX40	DB36, DB71, DB15, CVN, MGCD0103^, SNDX-275^, azacytidine^*	Angiogenesis	[66,67,96]
		Cell activation
		Immunoregulation
		Tumor necrosis
LAG-3	IMP32, BMS986016	T-Cell proliferation	[77]
LAG-3	IMP32, BMS986016	Cell maturation & activation	[77]
TIM-3	TSR-022, Sym023, ATIK2a	Immune response	[77,78,84,97-99]
		Tumorigenesis
		Cell invasion & activation
		Cell regulation
B7-H3	c-MYC SMIs, vorinostat^, DZNep^	Migration	[89]
		Angiogenesis
		T-Cell response
		Immune response
		Mediated signaling
		Promotes the cell cycle

Epigenetic SMI.