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Table 2 Epigenetic therapies in past and ongoing trials open to FL patients

From: Evolving therapeutic landscape in follicular lymphoma: a look at emerging and investigational therapies

Treatment Target Publication/NCT# Phase Total n [FL] Median lines of prior therapy ORR%a [CR%] Median PFS (mos) Grade ≥ 3 AEs (%)b Approved
EZH2 inhibitors
Tazemetostat EZH2 [60] II 99 [99; MT 45, WT 45) 2 MT: 69 [13] WT: 35 [4] MT: 13.8 WT: 11.1 Nonec  + 
Tazemetostat + rituximab EZH2 NCT04762160 II NAd NAd NAd NAd NAd
Tazemetostat + lenalidomide + rituximab EZH2 NCT04224493 I NAd NAd NAd NAd NAd
HDAC inhibitors
Vorinostat Class 1 and 2 HDACs [62] II 50 [39] 1 49 [10] 20 Neutropenia [36], thrombocytopenia [23], lymphopenia [13], diarrhea [5], anorexia [7]
Vorinostat + rituximab Class 1 and 2 HDACs [64] II 28 [22] 2 41 [27] 18.8 Lymphopenia [25], thrombocytopenia [18], neutropenia [11], fatigue [32], thrombosis [14], dehydration [11], hyperglycemia [11] hypotension [7], PNA [7],
Mocetinostat HDAC 1,2,3,11 [66] II 72 [31] 4 11 [4] 26.3 Fatigue [24], neutropenia [15], thrombocytopenia [12], anemia [8]
DNMT inhibitors
5-azacytidine + R-CHOP DNMT1 [68] I 10 [3] 3 66 [33] NP Neutropenia [50], thrombocytopenia [40], anemia [20], abscess [10], anorexia [10], bacteremia [10], nausea [10]
PRMT inhibitors
GSK3326595 PRMT5 NCT02783300e I NAd NAd NAd NAd NAd
JNJ-64619178 PRMT5 NCT03573310e I NAd NAd NAd NAd NAd
BET inhibitors
CPI-0610 BRD2, BRD4 [74] I 44 [8] 4 12 [0] NP NP
  1. Abbreviations: AEs—adverse events; CR—complete response rate; MT—mutant EZH2; NP—not presented; ORR—overall response rate; PFS—progression-free survival; PNA—pneumonia; R-CHOP—rituximab, cyclophosphamide, doxorubicin, vincristine and prednisone; WT—wild type EZH2
  2. aResponse rates in FL subset
  3. bGrade ≥ 3 seen in at least 5% of all patients regardless of lymphoma subtype
  4. cNo grade ≥ 3 events occurred in greater than 5% of patients, thrombocytopenia [3], neutropenia [3], anemia [2]
  5. dNot available, clinical trials are ongoing
  6. efirst in human study enrolling patients with NHL or solid tumors