Abstract
TNG908 is a clinical stage MTA-cooperative PRMT5 inhibitor that leverages the synthetic lethal interaction between PRMT5 inhibition and MTAP deletion. TNG908 was discovered using structure-based design following an initial high-throughput screening campaign. TNG908 is 15X selective for MTAPnull cell lines over isogenic MTAPWT 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 TNG908 drives dose-dependent, MTAPnull-selective antitumor activity in xenograft models, including durable tumor regressions in models representing glioblastoma, non-small cell lung cancer (adenocarcinoma and squamous), mesothelioma, cholangiocarcinoma, urothelial carcinoma, and others.
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