mubritinib

Mubritinib is a small molecule protein kinase inhibitor that was originally developed by Takeda for the treatment of cancer, particularly HER2-positive solid tumors. It acts as a potent and selective inhibitor of the human epidermal growth factor receptor 2 (HER2/ERBB2) tyrosine kinase, displaying over 4000-fold selectivity compared to other kinases such as EGFR, FGFR, PDGFR, Jak1, Src, and Blk. Mubritinib has also been shown to inhibit mitochondrial electron transport chain (ETC) complex I activity in certain contexts—most notably in acute myeloid leukemia (AML), where its anti-leukemic effects are attributed to this mechanism rather than ERBB2 inhibition. The drug completed phase I clinical trials for solid tumors but appears to have been discontinued with no further development reported since around 2008. Investigational indications included breast neoplasm, lung neoplasm, ovarian neoplasm, renal neoplasm, pancreatic neoplasm, and AML[1][3][4][5][7].

Other names

mubritinib