Thursday, April 10, 2014
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Carbonic anhydrase IX (CAIX)-targeted
small molecule-drug conjugates
molecule conjugates could be useful for imaging and treating cancer. A series
of small molecule ligands of CAIX, which is overexpressed in many types of
cancer, were conjugated to fluorescent dyes or cytotoxic agents with a linker
molecule. In a mouse xenograft model of human renal cell carcinoma (RCC),
several CAIX-targeted ligands conjugated to fluorescent dye selectively
accumulated at the tumor site. In the model, a CAIX-targeted ligand
conjugated to the cytotoxic agent mertansine caused more potent tumor
growth inhibition than untargeted conjugates or the RCC drugs Nexavar
Next steps include studies to identify a lead candidate for clinical development.
Pfizer Inc. markets the
tyrosine kinase (RTK)
inhibitor Sutent to treat gastrointestinal stromal tumors (GISTs), pancreatic
neuroendocrine tumors and advanced RCC.
and Bayer AG market
Nexavar to treat hepatocellular carcinoma and advanced RCC.
Published online April 10, 2014
Patented; licensing status
Krall, N. et al. Angew.
Chem. Int. Ed.; published online March 12, 2014;
Contact: Dario Neri, Swiss Federal Institute of Technology
Zurich (ETHZ), Zurich, Switzerland
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