Table 2.

Combination partners that have shown synergism with BET inhibitors in preclinical tumor models

ClassesSecond compoundExperimental disease model
Small molecules
ALK inhibitorsLymphoma (31)
BTK inhibitorsLymphoma (28, 31, 35, 36, 100, 101, 114)
CDK inhibitorsLymphoma (100, 101), osteosarcoma (51)
BCL2/MCL1 inhibitorsALL (115), AML (29, 116), LC (117), lymphoma (99–101)
EGFR/ERBB2 inhibitorsBC (97)
FLT3 inhibitorsAML (118)
Hedgehog inhibitorsLymphoma (31)
JAK inhibitorsAML (119)
MEK/ERK inhibitorsLymphoma (120), OC (91)
mTOR inhibitorsBC (40), glioblastoma (121), lymphoma (28, 35, 36, 114), osteosarcoma (122)
PARP inhibitorsBC (96), OC (96)
PI3K inhibitors, pan or selectiveBC (95), CC (95), lymphoma (28, 36, 102), glioblastoma (95), OC (90, 95)
Proteasome inhibitorsMM (116, 123)
Antibodies
Anti-CD20 monoclonal antibodiesLymphoma (36, 114, 124)
Immune modulators
Immunomodulatory drugs (IMiD)Lymphoma (36, 125, 126), MM (45)
Anti–PD-1 monoclonal antibodiesLymphoma (30)
Anti–4-1BB monoclonal antibodiesLymphoma (30)
Chimeric antigen receptor (CAR) T cellsALL (105)
Epigenetic drugs
EZH2 inhibitorsLymphoma (35, 127)
HDAC inhibitorsAML (128), BC (129), LC (130), lymphoma (31, 36, 101, 114, 131), melanoma (132), neuroblastoma (133), PC (134)
AzacytidineAML (116)
DecitabineLymphoma (36)
Chemotherapy
TemozolomideGlioblastoma (121)
Hormone therapy
AntiandrogenPrC (49)
Estrogen receptor degraderBC (135)
  • Abbreviations: ALL, acute lymphoblastic leukemia; AML, acute myeloid leukemia; BC, breast cancer; CC, colorectal cancer; LC, lung cancer; MM, multiple myeloma; OC, ovarian cancer; PC, pancreatic cancer, PrC; prostate cancer.