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Drug platforms

Carbonic anhydrase IX (CAIX)-targeted small molecule-drug conjugates

CAIX-targeted small 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 sorafenib or Sutent sunitinib. Next steps include studies to identify a lead candidate for clinical development.
Pfizer Inc. markets the receptor tyrosine kinase (RTK) inhibitor Sutent to treat gastrointestinal stromal tumors (GISTs), pancreatic neuroendocrine tumors and advanced RCC.
Amgen Inc. and Bayer AG market Nexavar to treat hepatocellular carcinoma and advanced RCC.

SciBX 7(14); doi:10.1038/scibx.2014.414
Published online April 10, 2014

Patented; licensing status undisclosed

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