Drug intelligence / Profile preview

DBPR114

Development stage
Phase 1
Lead developer
LaunXP Biomedical
Modality
Small Molecules
Administration
Oral
01

Overview

DBPR114 is a **novel small molecule multikinase inhibitor** designed for anticancer therapy[1][2][4][7]. It potently inhibits more than 57 oncogenic kinases, notably including **Aurora kinases (AURKA, AURKB)**, **FLT3**, **RET**, **KIT**, **TRKA**, **PDGFR beta**, **VEGFR1**, **VEGFR2**, **TYRO3/RSE**, **CSF1R**, **MET**, **TEK**, **PTK2B/PYK2**, and **EPHA4**, among others[7]. Its mechanism of action encompasses blocking cell proliferation, inducing apoptosis, causing cell cycle arrest, and inhibiting angiogenesis via downregulation of kinase phosphorylation and active receptor tyrosine kinases[1][2][4][7]. DBPR114 was initially developed as a dual FLT3/Aurora kinase inhibitor for **acute myeloid leukemia**, but has demonstrated broad-spectrum antitumor activity against advanced hepatocellular carcinoma (HCC), colon, stomach, lung, pancreas, uterine sarcoma, and gastric cancers[2][7]. It is particularly noteworthy for efficacy against **sorafenib-intrinsic and -acquired resistant HCC tumors**, and significantly prolongs survival and delays regrowth compared to regorafenib in preclinical models[1][2][4].

Other names
DBPR-114DBPR114DBPR 114
02

Targets

AXL (AXL receptor tyrosine kinase)AURKA (Aurora kinase A)AURKB (Aurora kinase B)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)RET (Rearranged during transfection receptor tyrosine kinase)TEK (Tie2)EPHA4CSF1R (Macrophage colony-stimulating factor receptor)NTRK1 (Tropomyosin-related receptor kinase A)PDGFRB (Platelet-derived growth factor receptor beta)PTK2BRPS6KA2 (Ribosomal protein S6 kinase alpha-2)TYRO3 (TYRO3 protein tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)

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