Drug intelligence / Profile preview

IAG933

Development stage
Phase 1
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

IAG933 is a small molecule inhibitor that targets the interaction between Yes-associated protein (YAP) and TEA domain transcription factors (TEAD), disrupting the YAP/TAZ–TEAD protein-protein interaction. This mechanism inhibits oncogenic activation of the Hippo pathway, which is implicated in tumor growth and metastasis in various solid tumors. Preclinical studies have shown that IAG933 can induce deep tumor regression in Hippo-driven mesothelioma xenografts and demonstrates efficacy both as monotherapy and in combination with MAPK/KRAS inhibitors for lung, pancreatic, and colorectal cancers. The drug is being developed primarily for advanced mesothelioma, tumors with NF2/LATS1/LATS2 mutations or functional YAP/TAZ fusions, and other solid tumors[1][4][5][7].

02

Targets

YAP1 (YES-associated protein–transcriptional enhancer factor domain complex)

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