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    DRUG:

    IAG933

    i
    Other names: IAG933, IAG-933, IAG 933
    Company:
    Novartis
    Drug class:
    TEAD inhibitor
    Related drugs:
    2ms
    A Phase I Study of IAG933 in Patients With Advanced Mesothelioma and Other Solid Tumors (clinicaltrials.gov)
    P1, N=156, Recruiting, Novartis Pharmaceuticals | Trial completion date: Oct 2025 --> Jan 2026 | Trial primary completion date: Oct 2025 --> Jan 2026
    Trial completion date • Trial primary completion date • Metastases
    |
    LATS1 (Large Tumor Suppressor Kinase 1) • LATS2 (Large Tumor Suppressor Kinase 2)
    |
    LATS1 mutation • LATS2 mutation
    |
    IAG933
    8ms
    Direct and selective pharmacological disruption of the YAP-TEAD interface by IAG933 inhibits Hippo-dependent and RAS-MAPK-altered cancers. (PubMed, Nat Cancer)
    Importantly this also extended to larger tumor indications, such as lung, pancreatic and colorectal cancer, in combination with RTK, KRAS-mutant selective and MAPK inhibitors, leading to more efficacious and durable responses. Clinical evaluation of IAG933 is underway.
    Journal
    |
    KRAS (KRAS proto-oncogene GTPase)
    |
    KRAS mutation
    |
    IAG933
    8ms
    A Phase I Study of IAG933 in Patients With Advanced Mesothelioma and Other Solid Tumors (clinicaltrials.gov)
    P1, N=156, Recruiting, Novartis Pharmaceuticals | Trial completion date: May 2025 --> Oct 2025 | Trial primary completion date: May 2025 --> Oct 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    LATS1 (Large Tumor Suppressor Kinase 1) • LATS2 (Large Tumor Suppressor Kinase 2)
    |
    LATS1 mutation • LATS2 mutation
    |
    IAG933
    1year
    A Phase I Study of IAG933 in Patients With Advanced Mesothelioma and Other Solid Tumors (clinicaltrials.gov)
    P1, N=156, Recruiting, Novartis Pharmaceuticals | Trial completion date: Sep 2024 --> May 2025 | Trial primary completion date: Sep 2024 --> May 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    LATS1 (Large Tumor Suppressor Kinase 1) • LATS2 (Large Tumor Suppressor Kinase 2)
    |
    LATS1 mutation • LATS2 mutation
    |
    IAG933
    over1year
    IAG933, a selective and orally efficacious YAP1/WWTR1(TAZ)-panTEAD protein-protein interaction inhibitor with pre-clinical activity in monotherapy and combinations (AACR 2023)
    Here we report the identification of IAG933, the first molecule able to potently and directly disrupt the YAP/TAZ-TEADs PPI with suitable properties to enter in clinical trial. Moreover, we provide evidence for combination benefits of IAG933 with several MAPK/KRAS inhibitors, both in vitro and in vivo, in non-Hippo altered models including lung, pancreatic and colorectal cancer. Overall, our results provide a rationale of progressing IAG933 as a monotherapy in patients with Hippo-mutated cancers, and as a combination partner in MAPK-dependent cancers, with the potential to treat patient populations of high unmet medical need.
    Preclinical • Late-breaking abstract
    |
    KRAS (KRAS proto-oncogene GTPase) • NF2 (Neurofibromin 2) • YAP1 (Yes associated protein 1) • WWTR1 (WW Domain Containing Transcription Regulator 1) • TAFAZZIN (Tafazzin) • VGLL4 (Vestigial Like Family Member 4)
    |
    IAG933 • Undisclosed YAP/TAZ-TEAD inhibitor