Table 3.
Combined use of BETi and other drugs in hematologic tumors.
| Hematological malignancy | BETi or BET-PROTAC | Type of combination agent | References |
|---|---|---|---|
| AML | JQ1 | Pan-HADCi, panobinostat | 67 |
| FLT3-ITD + AML | JQ1 | FLT3-TKI, AC220 (quizartinib) | 69 |
| FLT3-ITD + AML | PLX51107 | FLT3-TKI, quizartinib | 70 |
| AML | CPI203 | MDM2i, Idasanutlin/RG7388 | 72 |
| sAML | JQ1 | JAKi, ruxolitinib. HSP90i, AUY922 | 73 |
| AML | ABBV-744 | BCL-2 antagonists, venetoclax | 77 |
| AML/MDS | JQ1 | Hypomethylating agents, azacitidine | 79 |
| T-ALL | JQ1 | BCL-2 antagonists, venetoclax | 82 |
| CLL | GS-5829 | BTKi, ibrutinib; PI3Ki idelalisib | 84 |
| DHL/THL | I-BET | Pan-HDACi, vorinostat | 85 |
| RT-DLBCL | ARV-771 | BTKi, ibrutinib | 90 |
| MCL | JQ1 | BTKi, ibrutinib; HDACi, Panobinostat | 92 |
| MCL | CPI203 | immunomodulators, lenalidomide | 94 |
| CTCL | OTX015 | HDACi, Romidepsin | 97 |
| CTCL | mivebresib | JAKi, ruxolitinib | 98 |
| BL | OTX015 | PI3Ki idelalisib, CDKi SNS-032 and mTORi everolimus | 100 |
| BL | JQ1 | HDACi, Romidepsin | 101 |
| WM | JQ1 | Pan-HDACi, Panobinostat; BTKi, ibrutinib | 102 |
| PEL | JQ1 | immunomodulators, lenalidomide | 103 |
| MM | OTX015 | proteasome inhibitors, lenalidomide, and melphalan | 111 |
| MM | ARV-825 and ARV-763 | dexamethasone, mTORi everolimus and Akti afuresertib | 112 |
| Myc-induced lymphoma | RVX2135 | HDACi, Vorinostat and RVX2135 | 115 |
| DLBCL | PLX51107 and PLX2853 | BCL-2 antagonists, venetoclax | 121 |
| AML | ABBV-075 | BCL-2 antagonists, venetoclax | 122 |
| DLBCL | OTX015 | BTKi, ibrutinib | 125 |
| DLBCL, BL | JQ1, CPI-203 | mTORi everolimus, AKTi MK-2206, PI3Ki CAL-101. | 126 |
| Myc-induced lymphoma | JQ1, RVX2135 | ATRi, AZ20 | 128 |