Table 6 Inhibitors of PcG proteins undergoing current clinical trials in malignant cellsa.
From: Structural heterogeneity of the mammalian polycomb repressor complex in immune regulation
Target polycomb subunit | Agent | Mode of action | NCT ID | Phase | Target tumor types | Status |
|---|---|---|---|---|---|---|
EZH2 | Tazemetostat (EPZ-6438) | S-adenosyl- L-methionine (SAM) competitive inhibitor | NCT02875548 | II | Diffuse large B cell lymphoma | Recruiting |
NCT02601950 | II | INI (hSNF5; SMARCB1)-negative tumor and relapsed/refractory synovial sarcoma | Recruiting | |||
NCT01897571 | I/II | Advanced solid tumor and B cell lymphoma | Active, not recruiting | |||
NCT02601937 | I | INI (hSNF5; SMARCB1)-negative tumor and synovial sarcoma | Recruiting | |||
NCT02860286 | II | Malignant mesothelioma | Completed | |||
NCT03213665 | II | Relapsed/refractory advanced solid tumor and non-Hodgkin’s lymphoma | Recruiting | |||
NCT02889523 | Ib/II | Diffuse large B cell lymphoma | Suspended | |||
NCT03217253 | I | Metastatic or unresectable solid tumor | Active,not recruiting | |||
NCT03348631 | II | Recurrent ovarian cancer | Suspended | |||
GSK2816126 | SAM competitive inhibitor | NCT02082977 | I | Relapsed/refractory diffuse large B cell lymphoma and transformed follicular lymphoma | Terminated | |
CPI-1205 | SAM competitive inhibitor | NCT02395601 | I | B cell lymphoma | Completed | |
CPI-0209 | Second generation inhibitor of EZH2 | NCT04104776 | I/II | Advanced solid tumor | Recruiting | |
PF-06821497 | SAM competitive inhibitor | NCT03460977 | I | Relapsed/refractory small cell lung cancer,castration-resistant prostate cancer, and follicular lymphoma | Recruiting | |
SHR2554 | SAM competitive inhibitor | NCT03603951 | I | Relapsed/refractory mature lymphoid neoplasm | Recruiting | |
EZH1 and EZH2 | DS-3201b (Valemetostat tosylate) | SAM competitive inhibitor | NCT04102150 | II | Relapsed/refractory adult T cell leukemia/lymphoma | Recruiting |
EED | MAK683 | Binds to EED and change overall shape of PRC2 | NCT02900651 | I/II | Diffuse large B cell lymphoma | Recruiting |
BMI1 | PTC-596 | Phosphorylation of BMI-1 at two N-terminal sites which leads to the degradation of BMI-1 | NCT03605550 | Ib | High grade glioma and diffuse intrinsic pontine glioma | Recruiting |
NCT03206645 | I | Ovarian cancer | Recruiting | |||
NCT02404480 | I | Advanced solid cancer | Completed | |||
NCT03761095 | I | Leiomyosarcoma | Recruiting |
