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 Kadmon Corporation (originally ''Kadmon Pharmaceuticals'') is a biopharmaceutical company based in New York City. It also has operations in Warrendale, PA and Brighton, MA. The company was founded in 2009 by Samuel D. Waksal, founder and former ...

. Tesevatinib binds to and inhibits several

tyrosine -Tyrosine or tyrosine (symbol Tyr or Y) or 4-hydroxyphenylalanine is one of the 20 standard amino acids that are used by cells to synthesize proteins. It is a non-essential amino acid with a polar side group. The word "tyrosine" is from the Gr ...

receptor

kinase In biochemistry, a kinase () is an enzyme that catalyzes the transfer of phosphate groups from high-energy, phosphate-donating molecules to specific substrates. This process is known as phosphorylation, where the high-energy ATP molecule don ...

s that play major roles in tumor cell proliferation and tumor

vascularization Angiogenesis is the physiological process through which new blood vessels form from pre-existing vessels, formed in the earlier stage of vasculogenesis. Angiogenesis continues the growth of the vasculature by processes of sprouting and splitting ...

, including

epidermal growth factor receptor The epidermal growth factor receptor (EGFR; ErbB-1; HER1 in humans) is a transmembrane protein that is a receptor for members of the epidermal growth factor family (EGF family) of extracellular protein ligands. The epidermal growth factor recept ...

(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 Phase II, Phase 2 or Phase Two may refer to: Media * Marvel Cinematic Universe: Phase Two, six American superhero films from 2013–2015 * ''Star Trek: Phase II'', an unrealized television series based on the characters of Gene Roddenberry's ''S ...

clinical trials for the treatment of polycystic kidney disease in adults and children.

References

Angiogenesis inhibitors Experimental cancer drugs Tyrosine kinase inhibitors {{antineoplastic-drug-stub