Article
Tarloxotinib Is a Hypoxia-Activated Pan-HER Kinase Inhibitor Active Against a Broad Range of HER-Family Oncogenes.
Clinical cancer research : an official journal of the American Association for Cancer Research - 1 Mar 2021
Estrada-Bernal Adriana, Le Anh T, Doak Andrea E, Tirunagaru Vijaya G, Silva Shevan, Bull Matthew R, Smaill Jeff B, Patterson Adam V, Kim Chul, Liu Stephen V, Doebele Robert C
Abstract excerpt
PURPOSE: Approved therapies for EGFR exon 20, ERBB2 mutations, and NRG1 fusions are currently lacking for non-small cell lung cancer and other cancers. Tarloxotinib is a prodrug that harnesses tumor hypoxia to generate high levels of a potent, covalent pan-HER tyrosine kinase inhibitor, tarloxotinib-effector (tarloxotinib-E), within the tumor microenvironment. This tumor-selective delivery mechanism was designed...
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