BPI-460372 / Betta Pharma - LARVOL DELTA

The selective Yap/Tead inhibitor TY-1054 re-sensitizes acquired resistance to multiple tyrosine kinase-based targeted therapies (AACR 2025) - P1 | "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

In vitro and In vivo Drug Metabolism Analysis of BPI-460372 - A Covalent TEAD1/3/4 Inhibitor. (PubMed, Curr Drug Metab) - "This study elucidated the metabolism of BPI-460372 and provided a basis for pharmacokinetic and toxicological species selection, human pharmacokinetics prediction, and assessment of clinical co-administration limitations and possible metabolic pathways in humans."

Journal • Preclinical • Oncology • CYP1A2 • CYP3A4 • TEAD1

Development and validation of a UPLC-MS/MS method for rapid and simultaneous quantification of BPI-460372 and its metabolites BPI-460444 and BPI-460456 in human plasma. (PubMed, J Chromatogr B Analyt Technol Biomed Life Sci) - "The established analytical method showed great sensitivity, simplicity, accuracy, and reliability for the rapid and simultaneous analysis of the TEAD target inhibitor BPI-460372, alongside its major metabolites BPI-460444 and BPI-460456 in human plasma. This analytical method provided essential support for future clinical investigations and pharmacokinetic analysis."

Journal • Oncology • Solid Tumor

BPI-460372, a covalent, irreversible TEAD inhibitor in Phase I clinical development (AACR 2024) - "Thus, alternative dosing schedule could further improve the therapeutic window and enable combination studies in clinical development. Collectively, these results support further development of BPI-460372 for the treatment of cancers harboring Hippo pathway alterations."

Clinical • P1 data • Oncology

A Study of BPI-460372 in Advanced Solid Tumor Patients (clinicaltrials.gov) - P1 | N=82 | Recruiting | Sponsor: Betta Pharmaceuticals Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open • Oncology • Solid Tumor • LATS1

Tianfeng Securities: Give Betta Pharmaceuticals an overweight rating [Google translation] (Securities Star) - "On August 26, Beida Pharmaceutical Company released its 2023 semi-annual report...Ensartinib has been included in the medical insurance catalog for both first- and second-line treatment indications, resulting in a significant increase in product sales. In the first half of 2023, sales increased by 12.02% year-on-year....The clinical trial applications for BPI-460372, BPI-452080, BPB-101, and BPI-472372 projects have been approved by the National Medical Products Administration (NMPA) and can begin. The clinical trial of the BPI-460372 project has been approved by the NMPA and the US Food and Drug Administration (FDA)."

IND • New trial • Sales • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Discovery of BPI-460372, a potent and selective inhibitor of TEAD for the treatment of solid tumors harboring Hippo pathway aberrations (AACR 2023) - "In conclusion, BPI-460372 is a potent and selective TEAD palmitoylation inhibitor for the treatment of solid tumors harboring Hippo pathway aberrations. It is planned to enter Phase I clinical trial in China in early 2023."

Brain Cancer • CNS Tumor • Lung Cancer • Meningioma • Mesothelioma • Non Small Cell Lung Cancer • Oncology • Sarcoma • Soft Tissue Sarcoma • Solid Tumor • CCN1 • CTGF • LATS1

Phase 1 Study of BPI-460372 in Advanced Solid Tumor Patients (clinicaltrials.gov) - P1 | N=82 | Not yet recruiting | Sponsor: Betta Pharmaceuticals Co., Ltd.

Metastases • New P1 trial • Lung Cancer • Oncology • Solid Tumor • LATS1

Betta Pharmaceuticals (300558.SZ): BPI-460372 Tablets Approved for Clinical Trials with Advanced Solid Tumors [Google translation] (Zhitong Finance) - "Zhitong Finance APP News, Betta Pharmaceuticals...issued an announcement that the company received the 'Notice of Drug Clinical Trial Approval' (notification number: 2023LP00011, 2023LP00012) issued by the National Medical Products Administration ('NMPA'), The clinical trial of BPI-460372 tablets declared by the company has been approved by NMPA."

New trial • Oncology • Solid Tumor