The drug was first developed by Exelixis, Inc.[1] 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).

[2] The drug activity was initially studied in non-small cell lung cancer.

[4] In polycystic kidney disease, a histological study of the drug effects and toxicity in rats and mice was published in July 2017.

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