Drug intelligence / Profile preview

tinengotinib

Development stage
Phase 3
Lead developer
TransThera Biosciences
Modality
Small Molecules
Administration
Oral
01

Overview

Tinengotinib is an orally available small molecule multi–kinase inhibitor with antineoplastic and immunomodulatory activity. It selectively inhibits Aurora kinases A and B (AKs), Janus kinases (JAKs), fibroblast growth factor receptors (FGFRs 1–3), and vascular endothelial growth factor receptors (VEGFRs). By targeting these kinases—key drivers of cell proliferation, angiogenesis, and immune response modulation—tinengotinib disrupts tumor cell division and neovascularization in a variety of cancer types. It has demonstrated promising efficacy in advanced or metastatic solid tumors including cholangiocarcinoma with FGFR alterations refractory to prior FGFR inhibitors. Tinengotinib is under investigation in phase II/III clinical trials for cholangiocarcinoma and other solid tumors.[1][5][6][7][8][9][10]

Other names
TINENGOTINIB [INN]UNII-WZ9TJ0L9Y8UNII-WZ-9TJ0L9Y8UNII-WZ 9TJ0L9Y84-(5-(2-Chlorophenyl)-3-Methyl-2,10-Dihydropyrazolo[4,3-B] Pyrido[4,3-E][1,4]Diazepin-8-Yl) Morpholine5-(2-chlorophenyl)-3-methyl-8-(morpholin-4-yl)-1,10-dihydropyrazolo[4,3-b]pyrido[4,3-e][1,4]diazepine
02

Targets

CSF1R (Macrophage colony-stimulating factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)JAK2 (Janus kinase 2)FGFR3 (Fibroblast growth factor receptor 3)FGFR1 (Fibroblast growth factor receptor 1)VEGFR4 (Vascular endothelial growth factor Receptor-3)AURKB (Aurora kinase B)AURKA (Aurora kinase A)JAK1 (Janus kinase 1)FGFR2 (Keratinocyte growth factor receptor)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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