TAK-285

TAK-285 is an orally bioavailable, small molecule dual kinase inhibitor that selectively and potently inhibits human epidermal growth factor receptor 1 (EGFR/ErbB1) and human epidermal growth factor receptor 2 (HER2/ErbB2). By binding to and inhibiting the kinase activity of EGFR and HER2, TAK-285 blocks downstream signaling pathways involved in tumor cell proliferation, survival, angiogenesis, and metastasis. This mechanism may result in inhibition of tumor growth and regression in tumors overexpressing EGFR or HER2. Notably, TAK-285 is not a substrate for the p-glycoprotein (Pgp) efflux pump and has demonstrated central nervous system penetration in preclinical models, suggesting potential utility against brain metastases. The drug was developed by Takeda Pharmaceutical Company for the treatment of solid tumors but clinical development was discontinued after phase I trials due to strategic reasons[1][2][5][6][7].

Other names

N-(2-(4-((3-chloro-4-(3-(trifluoromethyl)phenoxy)phenyl)amino)-5H-pyrrolo(3,2-d)pyrimidin-5-yl)ethyl)-3-hydroxy-3-methylbutanamideUNII-70CCB438L6UNII70CCB438L6UNII 70CCB438L6871026-44-7