metatinib tromethamine (BMS-794833) / Simcere - LARVOL DELTA

BMS-794833 reduces anlotinib resistance in osteosarcoma by targeting the VEGFR/Ras/CDK2 pathway. (PubMed, J Bone Oncol) - "Recently, several TKIs, for instance regorafenib and cabozantinib, have showed clinical interest in treating osteosarcoma and target both vascular endothelial growth factor receptor (VEGFR) and mesenchymal epithelial transition factor (c-MET)...More importantly, BMS-794833 and anlotinib exerted synergistic therapeutic effects against osteosarcoma in vivo. Altogether, this study reveals a new (VEGFR)-targeting drug that can be combined with anlotinib for the treatment of osteosarcoma, which provides an important theoretical basis for overcoming anlotinib resistance."

Journal • Oncology • Osteosarcoma • Sarcoma • Solid Tumor • MET

BMS794833 inhibits macrophage efferocytosis by directly binding to MERTK and inhibiting its activity. (PubMed, Exp Mol Med) - "These data show that BMS794833 is a type II MERTK inhibitor that regulates macrophage efferocytosis. In addition, the real-time efferocytosis monitoring technology developed in this study has great potential for future applications."

Journal • Oncology • MERTK

Polypharmacological reprogramming of tumor-associated macrophages towards an inflammatory phenotype. (PubMed, Cancer Res) - "The effect of BMS-794833 was independent of its primary targets (MET and VEGFR2) but was dependent on its effect on multiple signaling pathways, including focal adhesion kinases, SRC family kinases, STAT3, and p38 MAP kinases. Collectively, these findings underline the efficacy of polypharmacological strategies in reprogramming complex signaling cascades activated during TAM polarization."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • KDR • STAT3

Safety, Efficacy, and Pharmacokinetics of Metatinib Tromethamine Tablet in Patients with Advanced Refractory Solid Tumors: A Phase I Clinical Trial. (PubMed, Oncologist) - "Metatinib administration of 200 mg/day was well tolerated, safe, and effective. The MTD was 200 mg/day, which should be recommended in further investigations."

Clinical • Journal • P1 data • PK/PD data • Gastrointestinal Cancer • Hepatocellular Cancer • Hepatology • Liver Failure • Oncology • Solid Tumor • KDR • MET