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Derazantinib

 
 

Derazantinib is an orally administered small-molecule inhibitor of the FGFR family of kinases and was developed by ArQule for the potential treatment of various solid tumors. Basilea entered into a license agreement with ArQule for the drug to research, develop, manufacture and exclusively commercialize derazantinib worldwide, excluding the People's Republic of China, Taiwan, Hong Kong and Macau.

Derazantinib is currently in a registrational clinical study for FGFR2 fusion positive intrahepatic cholangiocarcinoma (iCCA), a form of biliary tract cancer. In January 2019, Basilea reported results of an interim analysis from this study.  

At the end of January 2019, Basilea entered into a collaboration with Roche to explore a combination of derazantinib and Roche's PD-L1-blocking immune-checkpoint inhibitor atezolizumab (Tecentriq®) in patients with urothelial cancer (bladder cancer). 

FGFR alterations have been identified as potentially important therapeutic targets for various cancers, including iCCA, bladder, breast, gastric and lung cancers.1 Current scientific literature suggests FGFR alterations exist in a range of 5% to 30% in these cancers.2

References

1 R. Porta, R. Borea, A. Coelho et al. FGFR a promising druggable target in cancer: Molecular biology and new drugs. Critical Reviews in Oncology/Hematology 2017 (113), 256-267

2 T. Helsten, S. Elkin, E. Arthur et al. The FGFR landscape in cancer: Analysis of 4,853 tumors by next-generation sequencing. Clinical Cancer Research 2016 (22), 259-267

 
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