Drug intelligence / Profile preview

tesevatinib

Development stage
Phase 2
Lead developer
Kadmon
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Tesevatinib is an orally bioavailable small molecule inhibitor of multiple receptor tyrosine kinases (RTKs), including epidermal growth factor receptor (EGFR/ERBB1), human epidermal growth factor receptor 2 (HER2/ERBB2), vascular endothelial growth factor receptor (VEGFR), and ephrin type-B receptor 4 (EphB4). These RTKs are implicated in tumor cell proliferation and angiogenesis. Tesevatinib has demonstrated activity against tumors with EGFR mutations resistant to other EGFR inhibitors. It was initially developed for cancer indications such as non-small cell lung cancer (NSCLC) and glioblastoma but was also investigated for polycystic kidney disease due to its ability to inhibit molecular pathways central to the progression of PKD[1][2][3][6]. The drug was first developed by Exelixis and later acquired by Kadmon Corporation.

Other names
tesevatinib tosylate
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)EPHB4 (Ephrin type-B receptor 4)ERBB2 (Erb-b2 receptor tyrosine kinase 2)VEGFR (VEGFR family)

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