Table 4 |.
Summary of trials involving EZH2 inhibitors
| Drug | Trial phase (n) | Lymphoma subtype | Outcomes | Common grade ≥3 adverse events (% of patients) | Year | Refs or ClinicalTrials.gov identifier |
|---|---|---|---|---|---|---|
| Tazemetostat | I (21) | B cell NHL | ORR 38% and CR 14% | In 9% in total, including thrombocytopenia (3); neutropenia (3) | 2018 | 93 |
| Tazemetostat | II (165) | DLBCL and FL | ORR 40% in EZH2-mutant DLBCL and 18% in EZH2-wild-type DLBCL; ORR 63% in EZH2-mutant FL and 28% in EZH2--wild-type FL | In 18% in total | 2017 | 96 |
| Valemetostat | I (15) | NHL | ORR 53% and CBR 86%; TCL: 80% ORR | NR | 2017 | 95 |
| GSK2816126 | I (14) | NHL | DLBCL: 1 PR; FL: 1 SD | NR | 2016 | 94 |
| Tazemetostat + R-CHOP | Ib/II | DLBCL | Study ongoing | - | 2016 | NCT02889523 |
| Tazemetostat | II | B cell NHL | Study ongoing | - | 2016 | NCT02875548 |
| MAK683 | I/II | DLBCL | Study ongoing | - | 2016 | NCT02900651 |
| CPI-1205 | I | Lymphomas | Study ongoing | - | 2015 | NCT02395601 |
| Tazemetostat + atezolizumab | I | DLBCL | Study ongoing | - | 2014 | NCT02220842 |
CBR, clinical benefit rate; CR, complete response; DLBCL, diffuse large B cell lymphoma; EZH2, enhancer of zeste homologue 2; FL, follicular lymphoma; NHL, non-Hodgkin lymphoma; NR, not reported; ORR, overall response rate; PR, partial response; R-CHOP, rituximab, cyclophosphamide, doxorubicin, vincristine and prednisone; SD, stable disease; TCL, T cell lymphoma.