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Angiogenesis inhibitor
Tesevatinib
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    Tesevatinib

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    Tesevatinib
    Tesevatinib skeletal.svg
    Clinical data
    Routes of
    administration    		 Oral administration (tablets)
    Pharmacokinetic data
    Elimination half-life 50–70 hours
    Identifiers
    • N-(3,4-dichloro-2-fluorophenyl)-6-methoxy-7-{[(3aR,5r,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methoxy}quinazolin-4-amine
    CAS Number
    PubChem CID
    DrugBank
    ChemSpider
    UNII
    KEGG
    Chemical and physical data
    Formula C24H25Cl2FN4O2
    Molar mass 491.39 g·mol−1
    3D model (JSmol)
    • CN1C[C@H]2C[C@H](C[C@H]2C1)COc3cc4c(cc3OC)c(ncn4)Nc5ccc(c(c5F)Cl)Cl
    • InChI=1S/C24H25Cl2FN4O2/c1-31-9-14-5-13(6-15(14)10-31)11-33-21-8-19-16(7-20(21)32-2)24(29-12-28-19)30-18-4-3-17(25)22(26)23(18)27/h3-4,7-8,12-15H,5-6,9-11H2,1-2H3,(H,28,29,30)/t13-,14-,15+ checkY
    • Key:HVXKQKFEHMGHSL-QKDCVEJESA-N checkY

    Tesevatinib (KD019, XL647) is an experimental drug proposed for use in kidney cancer and polycystic kidney disease. The drug was first developed by Exelixis, Inc. and was later acquired by Kadmon Corporation. Tesevatinib binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including epidermal growth factor receptor (EGFR; ERBB1), epidermal growth factor receptor 2 (HER2; ERBB2), vascular endothelial growth factor receptor (VEGFR), and ephrin B4 (EphB4).

    The drug activity was initially studied in non-small cell lung cancer. In a 2007 pre-clinical study with xenograft tumors of an erlotinib-resistant cell line tesevatinib substantially inhibited the growth of these tumors. In polycystic kidney disease, a histological study of the drug effects and toxicity in rats and mice was published in July 2017.

    As of March 2019 the drug was in Phase II clinical trials for the treatment of polycystic kidney disease in adults and children.


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