Table 1:

Pipeline stage of small molecule immunotherapeutics

Small Molecule	Molecular Target	Pipeline Stage
BMS-1001	PD-L1 antagonist	Preclinical
BMS-1116	PD-L1 antagonist	Preclinical
CA-170	PD-L1/VISTA antagonist	Phase I(12)
CA-327	PD-L1/TIM-3 antagonist	Preclinical
Imiquimod	TLR7/8 agonist	Approved
Resiquimod	TLR7/8 agonist	Phase I/II(82)
852A	TLR7 agonist	Phase II(83)
VTX-2337	TLR8 agonist	Phase II(84)
ADU-S100	STING agonist	Phase I(85)
MK-1454	STING agonist	Phase I(86)
Ibrutinib	Btk/Itk inhibitor	Approved
3AC	SHIP1 inhibitor	Preclinical
Idelalisib	PI3K-δ inhibitor	Approved
IPI-549	PI3K-γ inhibitor?	Phase I(87)
Epacadostat	IDO inhibitor	Discontinued
AT-38	Arginase inhibitor	Preclinical
CPI-444	A2A receptor antagonist	Phase I/II(88)
Vipadenant	A2A receptor antagonist	Preclinical
Preladenant	A2A receptor antagonist	Phase I(89)
PBF 509	A2A receptor antagonist	Phase II(69)
AZD4635	A2A receptor antagonist	Phase I/II(90)
Galuniseritib	TGF-βR1 kinase/Alk5 inhibitor	Preclinical(91)
OTX015/ MK-8628	Bromodomain inhibitor	Phase II(92)
CPI-0610	Bromodomain inhibitor	Phase II(93)