Midostaurin, also known as PKC-412, PKC-412A and CGP 41251; is a synthetic indolocarbazole multikinase inhibitor with potential antiangiogenic and antineoplastic activities. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors. Midostaurin was approved in 2017.
Wang, Liping & Zhuang, Yibin & Kunlai, Sun & Zhu, Weiming. (2014). Synthesis and Cytotoxicity of Halogenated Derivatives of PKC-412. Chinese Journal of Organic Chemistry. 34. 1603. 10.6023/cjoc201403046.
Juhasz, Zsuzsa Potarine; Racz, Csilla Nemethe; Struba, Szabolcs; Ferenczi, Renata Kertine; Tamas, Tivadar. Solid state forms of Midostaurin. WO 2018165071. (Assignee Teva Pharmaceutical Works Ltd., Hung.; Teva Pharmaceuticals Usa, Inc.)
