Drug intelligence / Profile preview

merestinib

Development stage
Phase 2
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Merestinib is an orally available, investigational small molecule multi-targeted kinase inhibitor developed primarily for the treatment of various cancers. Its mechanism of action centers on inhibiting the proto-oncogene c-Met (hepatocyte growth factor receptor), as well as several other receptor tyrosine kinases including MST1R (RON), FLT3, AXL, MERTK, TEK (TIE2), ROS1, NTRK1/2/3 (neurotrophic tyrosine kinase receptors), and DDR1/2 (discoidin domain receptors). By targeting these kinases, merestinib exerts antiproliferative and antiangiogenic effects that may suppress tumor growth and progression. The drug has been evaluated in clinical trials for advanced solid tumors such as biliary tract cancer (including cholangiocarcinoma), non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma[2][6][7]. Developed by Eli Lilly with contributions from academic partners such as Dana-Farber Cancer Institute and Indiana University School of Medicine[3], merestinib remains investigational; several phase II studies have been terminated or completed without regulatory approval to date[8][10].

Other names
merestinibN-(3-fluoro-4-((1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide
02

Targets

AXL (AXL receptor tyrosine kinase)NTRK3 (Tropomyosin receptor kinase C)MET (Mesenchymal-epithelial transition factor receptor)MST1R (Recepteur d'origine nantais)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)TEK (Angiopoietin-1 receptor)DDR1 (Discoidin domain receptor 1)NTRK1 (Tropomyosin-related receptor kinase A)FLT3 (Fms related receptor tyrosine kinase 3)NTRK2 (Tropomyosin-related kinase receptor type B)DDR2 (Discoidin domain receptor tyrosine kinase 2)

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