Table 3.
Latency-Reversal Agents | Class | Stage | References |
---|---|---|---|
Romidepsin (FK228), Vorinostat (SAHA), Panobinostat(LBH589) | Histone deacetylase inhibitors | Clinical trial | NTC02092116 (65), NCT02092116 (65, 66), NCT01933594 (67, 68), NCT01319383 (68–71), NTC02092116 (65), NCT01365065 (72, 73), NCT03803605 (74), NCT02336074 (75), NCT01680094 (69, 76), NCT02471430 (76) |
Belinostat (PXD101), Givinostat (ITF2357), Nanatinostat(CHR-3996) | Histone deacetylase inhibitors | In vitro | (77, 78) |
Nicotinamide | Histone deacetylase inhibitors | Ex vivo | (79) |
JQ1, I-BET151, I-BET, MS417, UMB-136, OTX015, CPI-203, RVX-208, PFI-1, BI-2536, BI-6727, Apabetalone | Small-molecule bromodomain inhibitors | In vitro | (80–88) |
GSK-343, EPZ-6438 (Tazemetostat) | Small-molecule histone methyltransferase inhibitors targeted to EZH2 | In vitro | (89) |
UNC-0638 | Small-molecule histone methyltransferase inhibitors targeted to EHMT2 | In vitro | (89) |
EED226, A-395 | Small-molecule histone methyltransferase inhibitors targeted to EED | In vitro | (90) |
DZNep | Lysine-specific histone methyltransferase inhibitor targeted to EZH2 | In vitro | (91, 92) |
BIX-01294 | Lysine-specific histone methyltransferase inhibitor of the HKMT G9a | In vitro | (79, 92) |
Chaetocin | Lysine-specific histone methyltransferase inhibitor of the HKMT SUV39H1 | In vitro | (79, 92) |
5-AzaC, 5-AzadC | DNA methylation inhibitors | In vitro | (93) |
Ingenol, Bryostatin-1 | Protein kinase C activators | Clinical trial | NCT04503928 (94, 95), NCT02531295 (96–97), NCT02269605 (98) |
Prostratin | Protein kinase C activators | In vitro | (99) |
Tat-R5M4 | Toll-like receptor agonist | In vitro | (100) |
Pam3CSK4 | Toll-like receptor 1/2 agonist | In vitro | (101) |
GS-9620 | Toll-like receptor 7 agonist | Clinical trial | NCT02858401 (102) |
GS-986 | Toll-like receptor 7 agonist | In vivo | (103) |
R-848 | Toll-like receptor 7/8 agonist | In vitro | (104) |
3M-002 | Toll-like receptor 8 agonist | In vitro | (104) |
MGN 1703 | Toll-like receptor 9 agonist | Clinical trial | NCT02443935 (105, 106) |
CPG 7909 | Toll-like receptor 9 agonist | Clinical trial | NCT00562939 (107) |
nivolumab | Monoclonal antibodies targeting PD-1 | Case report | (108) |
pembrolizumab | Monoclonal antibodies targeting PD-1 | In vitro | (108) |
Ipilimumab | Monoclonal antibodies targeting CTLA-4 (CD152) | Case report | (109) |
BMS-936559 | Monoclonal antibodies targeting PD-L1 | Clinical trial | NCT02028403 (110) |
galectin-9 | Human carbohydrate-binding immunomodulatory protein | In vitro | (111) |
Procyanidin trimer C1 | MAPK agonist | In vitro | (80) |
Maraviroc | CCR5 antagonist | Clinical trial | NCT01365065 (112), NCT00795444 (113) |
N-803 | Interleukin-15 Superagonist | In vivo | (114) |
AZD5582, Ciapavir (SBI-0953294) | Activator of the non-canonical NF- κB pathway | In vivo | (115, 116) |
Disulfiram (C10H20N2S4) | Activators of Akt signaling pathway | Clinical trial | NCT01944371 (117) |
NF- κB, Nuclear Factor- κB; HKMT, histone-lysine methyltransferase; EHMT2, euchromatic histone-lysine N-methyltransferase 2; PD-1, programmed cell death protein; CTLA-4, cytotoxic T lymphocyte antigen 4; PD-L1, programmed cell death protein ligand 1.