Voegtle, Markus, Sellner, Holger, Chapeau, Emilie, Furet, Pascal, Salem, Bahaa, Le Douget, Mickael, Bordas, Vincent, Groell, Jean-Marc, Le Goff, Anne-Laure, Rouzet, Christine, Wietlisbach, Thomas, Zimmermann, Thomas-1, McKenna, Joseph, Brocklehurst, Cara, Chene, Patrick, Wartmann, Markus, Scheufler, Clemens, Kallen, Jörge, de Kanter, Ruben, Harflinger, Stephanie, Zecri, Frederic, Schmelzle, Tobias and Soldermann, Nicolas (2026) Discovery of Clinical Candidate IAG933, a Potent YAP-TEAD PPI Disrupter. Journal of medicinal chemistry. ISSN 1520-4804

Abstract

The interaction of transcriptional enhanced associate domain (TEAD) and transcriptional coactivator yes-associated protein (YAP) mediates oncogenic functions downstream of the Hippo pathway. In this report, we outline our efforts to find a potent inhibitor of this protein-protein interaction with suitable properties for clinical evaluation. We detail the medicinal chemistry program that led to the discovery of IAG933, an inhibitor with a balanced ADME profile, enabling its evaluation as a potential treatment option in clinical settings.

Item Type:	Article
Date Deposited:	20 Mar 2026 00:45
Last Modified:	20 Mar 2026 00:45
URI:	https://oak.novartis.com/id/eprint/58837