Table 1

Overview of the major histone methylation modifiers-targeted drugs and combination therapies with immune checkpoint blockades in clinical trials

CategoryEnzymeTargetDrugCancer typeNCT numberPhase
MLL1H3K4JNJ-75276617Acute leukemiaNCT04811560Ⅰ
KMTEZH1H3K27ValemetostatLeukemia/Lymphoma
Metastatic prostate, urothelial, and renal cell cancers		NCT04703192
NCT04842877
NCT04102150
NCT04388852		Ⅱ
Ⅱ
Ⅱ
Ⅰ
EZH2H3K27TazemetostatAdvanced soft tissue sarcoma
Relapsed/refractory follicular lymphoma
Head and neck squamous cell carcinoma
Urothelial carcinoma		NCT04204941
NCT04224493
NCT04624113
NCT03854474		Ⅲ
Ⅲ
Ⅰ
Ⅱ
CPI-1205+IpilimumabAdvanced solid tumorsNCT03525795Ⅰ
Tazemetostat+PembrolizumabAdvanced Urothelial CarcinomaNCT03854474Ⅰ/Ⅱ
SETD2H3K36EZM0414Multiple myeloma/Diffuse large B-Cell lymphomaNCT05121103Ⅰ
DOT1LH3K79PinometostatAcute myeloid leukemiaNCT03701295
NCT03724084		Ⅱ
Ⅱ
KDMLSD1H3K4/H3K9 Seclidemstat Advanced solid tumors
Myelodysplastic syndrome
Ewing or Ewing-related sarcoma
Select gynecologic cancers		NCT03895684
NCT04734990
NCT03600649
NCT04611139 		Ⅰ
Ⅱ
Ⅰ
Ⅰ
JBI-802Solid tumorsNCT05268666Ⅱ
BomedemstatMyeloproliferative neoplasm
Small cell lung cancer		NCT05223920
NCT05191797		Ⅱ
Ⅱ
CC-90011Acute myeloid leukemiaNCT04748848Ⅰ
CC-90011+NivolumabSmall cell lung cancer
Squamous non-small cell lung cancer		NCT04350463Ⅱ
INCB059872+PembrolizumabAdvanced or metastatic solid tumorsNCT02959437Ⅰ/Ⅱ
Bomedemstat+AtezolizumabSmall cell lung cancerNCT05191797Ⅰ/Ⅱ
INCB059872+NivolumabSolid tumors and hematologic malignancyNCT02712905Ⅰ/Ⅱ