Vopimetostat (TNG462, TNG-462) is a potent, selective, MTA-cooperative PRMT5 inhibitor, selective inhibits MTAP-deleted cancer cell lines.
TNG462 shows antiproliferative activity is selective for MTAP-deleted cells in vitro.
TNG462 is 45X selective for MTAP-deleted cancer cell lines over isogenic MTAP WT cell lines and has marked selectivity for MTAP-deleted cancer cell lines independent of lineage in a large, diverse cell line panel.
Oral administration of TNG462 drives dose-dependent antitumor activity including durable tumor regressions and complete responses in cell line- and patient-derived xenograft models representative of clinically relevant histologies.
