Drug intelligence / Profile preview

NPS-1034

Development stage
Preclinical
Lead developer
Hope Biosciences
Modality
Small Molecules
Administration
Oral
01

Overview

NPS-1034 is a small molecule **dual kinase inhibitor** that primarily targets the receptor tyrosine kinases **MET (hepatocyte growth factor receptor)** and **AXL**, with reported IC50 values of 48 nM for MET and 10.3 nM for AXL[8][13]. It also shows inhibitory activity toward other kinases, including mutant forms of MET and ROS1[7][4]. Mechanistically, NPS-1034 disrupts signaling pathways involved in cell proliferation, migration, survival, and epithelial-to-mesenchymal transition (EMT), notably suppressing the **MET/PI3K/AKT axis** and reducing tumor cell viability through induction of apoptosis[1][2][3][4]. Studies indicate it may additionally modulate immune responses by inducing type I interferon and TNF production via RIG-I and MDA-5 signaling pathways[1][2][3]. It has shown effects in vitro and in vivo in multiple cancer models, including pancreatic ductal adenocarcinoma, renal cell carcinoma, testicular cancer, gastric cancer, and non-small cell lung cancer—especially in overcoming resistance to EGFR tyrosine kinase inhibitors[1][2][3][4][5][6].

Brand names
NPS-1034NPS1034NPS 1034
Other names
NPS-1034NPS1034NPS 1034
02

Targets

AXL (AXL receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)TNFRSF1A (Tumor necrosis factor receptor superfamily member 1A)FLT3 (Fms related receptor tyrosine kinase 3)

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