IAG933 (IAG-933) is a potent, selective and orally efficacious YAP1/WWTR1(TAZ)-pan TEAD protein-protein interaction inhibitor (YAP/TAZ-TEADs PPI), inhibits TEAD-driven transcriptional activity and displays anti-cancer effects.
IAG933 specifically abrogates the interaction between YAP/TAZ coactivators and all four TEAD isoforms, thus selectively inhibiting TEAD-driven transcriptional activity and inducing anti-cancer effects.
IAG933 exhibits robust anti-tumor efficacy in cancer models bearing NF2 loss of function or expressing TAZ-fusions.
IAG933 also shows combination benefits with several MAPK/KRAS inhibitors, both in vitro and in vivo, in non-Hippo altered models including lung, pancreatic and colorectal cancer.
