TY-1054 / TYK Medicines - LARVOL DELTA

The selective YAP/TEAD inhibitor TY-1054 enhances the efficacy of KRAS inhibitors or Trop2-ADC in multiple solid tumors (AACR 2026) - "TY-1054 not only enhanced the efficacy of KRAS G12Di RMC-9805 in SU.86.86 (PDAC, KRAS G12D) in vitro and in vivo, but also enhanced the efficacy of pan-KRASi Daraxonrasib in SU.86.86 in vitro and in vivo...TY-1054 enhances cetuximab efficacy in head and neck squamous cell carcinoma (HNSCC) Cal33 cells...TY-1054 enhances the efficacy of Trop2-ADC (SKB264/Sac-TMT) in triple-negative breast cancer (TNBC) (MDA-MB 231 and HCC1806), NSCLC (H1975 and HCC827), and trastuzumab-resistant breast cancer (JIMT-1) cells... 1. TY-1054 not only enhanced the efficacy of FDA-approved KRAS G12C inhibitors, Adagrasib and Sotorasib, in Non-Small Cell Lung Cancer (NSCLC) H1373 and H2122 cells, but also enhanced the efficacy of Divarasib (GDC-6036) and pan-KRASi Daroxonrasib (RMC-6236) in NSCLC H1972 and H2122 cells. 2."

ADC • Clinical • Breast Cancer • Head and Neck Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • Triple Negative Breast Cancer • KRAS

The selective Yap/Tead inhibitor TY-1054 re-sensitizes acquired resistance to multiple tyrosine kinase-based targeted therapies (AACR 2025) - P1, P1/2 | "Small molecules that block auto-palmitoylation of TEADs, such as VT3989 (NCT04665206) and BPI-460372 (NCT05789602), have been successfully to enter the clinical trials. TY-1054 had excellent efficacy in the H226 CDX and HNSCC PDX mouse models. TY-9591 is a third-generation EGFR inhibitor developed by TYK Medicines and is currently under pivotal Phase III clinical investigation in China. Our studies showed that TY-9591 had excellent efficacy in the PC9 CDX mouse model, but tumors gradually recurred, as Osimertinib did."

Preclinical • Head and Neck Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma of Head and Neck

TYK Medicines…is pleased to announce that the research progress and results for five innovative drug projects under development of the Company, namely TY-0609 (CDK4 inhibitor), TY-2699a (CDK7 inhibitor), TY-2719 (EGFR/FAK (PROTAC) inhibitor), PI3Kα (PI3Kα inhibitor), and TY-1054 (YAP-TEAD inhibitor), will be presented by the Company in poster presentation at 2026…AACR annual meeting (HKEXnews)

Preclinical • Solid Tumor

Study of TYK-01054 Capsules in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=219 | Not yet recruiting | Sponsor: TYK Medicines, Inc

New P1/2 trial • Mesothelioma • Oncology • Solid Tumor

TY-1054 exerts antitumoral effects both in vitro and in vivo (Bioworld) - "TYK Medicines Inc. has presented a novel YAP/TEAD interaction inhibitor compound, TY-1054, as a potential approach for treating cancer with dysregulated Hippo/YAP pathway."

Preclinical • Oncology