Table 1.

Inhibitors targeting epigenetic oncogenic drivers in clinical development (active trials only).

Target	Biomarkers	Inhibitors	Indication	Clinical trial number
EZH2	EZH2 GOF mutation	Tazemetostat, GSK2816126, PF-06821497, FTX-6058, SHR2554)	B-cell Non-Hodgkin lymphoma, follicular lymphoma, solid tumors	NCT03456726 NCT05228158 NCT03603951 NCT03213665 NCT05467943 NCT04104776 NCT05551936 NCT04224493
		Tazemetostat, SHR2554, PF-06821497, Valmetostat, HH-2853	PTCL, MPNST, Breast cancer, TNBC, mCRPC, R/R B-cell NHL, R/R ATL	NCT05559008 NCT04355858 NCT03805399 NCT06122389 NCT04917042 NCT03460977 NCT04703192 NCT04842877 NCT04102150 NCT05633969 NCT06244485 NCT03930953 NCT04390737
EED	EZH2 GOF mutation	MAK-683, APG-5918, ORIC-944	DLBCL, solid tumors	NCT02900651 NCT05415098. NCT05413421
Menin	MLL rearrangements/ NPM1m/FLT3m	BMF-219, SNDX-5613, KO-539, DSP-5336 JNJ-75276617	Leukemia, R/R Leukemias, MRD-positive AML	NCT05153330 NCT04065399 NCT04067336 NCT04811560 NCT04988555 NCT05326516 NCT05453903 NCT05521087 NCT05406817 NCT05761171 NCT04065399 NCT05360160 NCT06284486 NCT06226571 NCT05886049 NCT06222580 NCT05735184 NCT06001788 NCT04988555
	KRAS mutation	BMF-219	CRC, NSCLC, PDAC	NCT05631574
	Hox upregulation	SNDX-5613	Leukemias	NCT06229912
		SNDX-5613	AML, Pediatric AML, CRC, Solid tumors	NCT06313437 NCT06177067 NCT05731947
NSD2	NSD2 translocation	KTX-1001	Multiple myeloma	NCT05651932
SMARCA2/4		FHD-286	Metastatic uveal melanoma, AML, MDS	NCT04879017 NCT04891757
KAT6A		PF-07248144	metastatic ER+HER2- breast cancer, CRPC, NSCLC	NCT04606446