altiratinib

Altiratinib is an orally bioavailable small molecule inhibitor targeting multiple receptor tyrosine kinases, including c-Met/hepatocyte growth factor receptor (HGFR), vascular endothelial growth factor receptor type 2 (VEGFR2), Tie2 receptor tyrosine kinase (TIE2), and tropomyosin receptor kinase (Trk). It was designed to address several hallmarks of cancer by inhibiting tumor initiation, progression, angiogenesis, invasion, metastasis, and drug resistance mechanisms in the tumor microenvironment. Altiratinib achieves this through balanced inhibition of MET, TIE2, and VEGFR2 by binding to their switch control pockets and inducing type II inactive conformations. The drug has demonstrated substantial blood-brain barrier penetration—an important property for treating brain cancers such as glioblastoma—and is being investigated primarily for solid tumors. Developed using Deciphera’s proprietary switch control kinase inhibitor platform, it inhibits both wild-type and mutant forms of MET[1][6][8].

Other names

altiratinib [USAN]