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Table 2 Ongoing EZH2 targeted clinical trials

From: EZH2 inhibition in ARID1A mutated clear cell and endometrioid ovarian and endometrioid endometrial cancers

Targeted Agent Trade Name Route Trial Tumor Status/Adverse Events (Grade 3–4) References
EPZ-6438 Tazemetostat PO Phase 1 NHL Thrombocytopenia
Neutropenia
Hypertension
Anorexia
Transaminitis
[58]
   PO Phase 1/2 B-cell lymphoma or advanced solid tumor Recruiting actively (Clinicaltrials.Gov. (2.13.2017)), (Epizyme pharmaceuticals website. (2.13.2017))
NCT01897571
Nausea
Asthenia
Thrombocytopenia
Neutropenia
Fatigue
   PO Phase 1 Pediatric INI1 negative tumors or synovial sarcoma Recruiting actively (Clinicaltrials.Gov. (2.13.2017)), (Epizyme pharmaceuticals website. (2.13.2017))
NCT02601937
   PO Phase 2 Adult INI1 negative tumors or synovial sarcoma Recruiting actively (Clinicaltrials.Gov. (2.13.2017)), (Epizyme pharmaceuticals website. (2.13.2017))
NCT02601950
   PO Phase 2 Malignant mesothelioma Recruiting actively (Clinicaltrials.Gov. (2.13.2017)), (Epizyme pharmaceuticals website. (2.13.2017))
NCT02860286
GSK 2,816,126 GSK126 IV Phase 1/2 Diffuse large B-cell lymphoma Fatigue [59]
Nausea
Vomiting
Anemia
EPZ-5676 Pinometostat IV Phase 1 Leukemia Hypophosphatemia [60]
Neutropenia
Reduced ejection fraction
Transaminitis
CPI-1205   IV Phase 1 B cell lymphoma Recruiting actively (Clinicaltrials.Gov. (2.13.2017)),
NCT02395601