Table 2.

Clinical evaluation of cancer‐associated transcription factor small molecule inhibitors

Target DNA binding protein	Inhibitor name	Company	Mode of action	Clinical trial no.	Reference
STAT3	Napabucasin	Boston Biomedical	Inhibition of target genes driven by STAT3	NCT02753127	35
CBP/β‐catenin	E7386	Eisai	Inhibition of Wnt target genes through modulation of β‐catenin/CBP interaction	NCT04008797	34
HIF2α	PT2385	Peloton Therapeutics	Allosteric inhibition of the dimerization of HIF2α with ARNT	NCT02293980	59
NF‐κB and GATA3	MLN9708	Millennium Pharmaceuticals	Proteasome inhibitor targeting NF‐κB and GATA3	NCT02181413	36
BRD4	AZD5153	AstraZeneca	Disruption of the chromatin binding activity of bromodomain‐containing protein 4	NCT03205176	37
EWS‐FLI1	TK216	Oncternal Therapeutics	Blocking of the physical interaction of E26 transformation‐specific transcription factors with RNA helicases	NCT02657005	38
MDM2	BI‐907828	Boehringer Ingelheim	Inhibition of physical interaction between MDM2 and p53	NCT03449381	60

DNA binding proteins, including fusion genes, are promising targets for cancer therapy and are currently being evaluated in clinical trials.

ARNT, aryl hydrocarbon receptor nuclear translocator; BRD4, bromodomain‐containing protein 4; CBP, CREB‐binding protein; EWS, Ewing's sarcoma; FLI1, friend leukemia virus integration 1; HIF‐2α, hypoxia‐inducible factor‐2α; MDM2, murine double minute homolog 2; NF‐κB, nuclear factor‐κB; STAT3, signal transducer and activator of transcription 3.