Description
KPT-276 is an orally bioavailable inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity.
In vivo, KPT-276 (150 mg/kg) increases survival and reduces spleen weight and white blood cell count in an MV4-11 acute myeloid leukemia (AML) mouse xenograft model. It also reduces tumor volume and increases survival in a BT 145 glioblastoma mouse xenograft model when administered at a dose of 75 mg/kg.
References
[1]. ranganathan p, yu x, na c, et al. preclinical activity of a novel crm1 inhibitor in acute myeloid leukemia. blood, 2012, 120(9): 1765-1773.
[2]. schmidt j, braggio e, kortuem km, et al. genome-wide studies in multiple myeloma identify xpo1/crm1 as a critical target validated using the selective nuclear export inhibitor kpt-276. leukemia, 2013, 27(12): 2357-2365.