tng260

TNG260 is a first-in-class, orally administered, highly selective small molecule inhibitor of the CoREST (Co-repressor of Repressor Element-1 Silencing Transcription) complex. It acts primarily by inhibiting the catalytic activity of histone deacetylase 1 (HDAC1) within the CoREST complex, leading to increased acetylation of chromatin histones, chromatin remodeling, and altered gene expression. This mechanism reprograms transcription in STK11-mutant cancer cells and modulates tumor cytokine secretion to favor immune-mediated tumor cell killing. TNG260 is being developed for use in combination with checkpoint inhibitors such as pembrolizumab to overcome resistance in STK11-mutant cancers—including non-small cell lung cancer (NSCLC), breast, cervical, pancreatic cancers, and carcinomas of unknown primary—by reversing immune evasion associated with STK11 loss-of-function mutations[1][2][3][4][5][6].

Other names

CoREST inhibitor TNG260