Pyrrolidine, also known as tetrahydropyrrole, is a saturated five-membered heterocyclic ring, which is miscible with water. Pyrrolidine exists in many alkaloids and drug molecules, such as kappa opioids, antagonists of dopamine D4 receptors, and HIV reverse transcriptase inhibitors.
IAG933 is a potent, selective, and first-in-class inhibitor from Novartis that directly inhibits the protein-protein interaction (PPI) between YAP/TAZ and TEAD. By blocking this PPI, IAG933 interferes with oncogenic functions downstream of the Hippo signaling pathway, particularly in mesothelioma and other tumors with NF2 loss-of-function mutations or YAP/TAZ fusions. This inhibition reduces transcriptional activity and induces cell death in cancer cells, leading to significant tumor regressions in xenograft models. Additionally, combining IAG933 preclinically with other targeted therapies (i.e., RTK, KRAS-mutant selective, and MAPK inhibitors) shows promise for improving the efficacy and durability of treatment responses. IAG933 is currently being evaluated in a Ph. I trial (NCT04857372) for solid tumors with Hippo pathway alterations. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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