CGP62221

CGP62221 is an active **O-demethylated metabolite** of the oral multi-targeted kinase inhibitor midostaurin. Midostaurin is metabolized primarily by hepatic CYP3A4 to produce CGP62221, which retains pharmacologic activity. While CGP62221 specifically blocks c-kit-dependent mast cell proliferation and inhibits IgE-mediated histamine release, it is also implicated in broad spectrum inhibition of kinase signaling pathways *in vitro*. The metabolite exhibits a markedly prolonged elimination half-life and is >99.8% bound to plasma proteins, mostly α1-acid glycoprotein. CGP62221 is under investigation as part of midostaurin therapy for malignancies such as acute myeloid leukemia and systemic mastocytosis[1][2][4][5].

Other names

O-demethylated midostaurin