Verdinexor is an orally bioavailable selective inhibitor of nuclear export (SINE), inhibits nuclear export protein Exportin 1 (XPO1/CRM1) against canine tumor cell lines and also reduce influenza virus replication in vitro and in vivo.
Verdinexor (KPT-335) is an innovative, orally-administered selective inhibitor of nuclear export (SINE) that blocks the nuclear export protein Exportin 1 (XPO1/CRM1), showing efficacy against canine cancer cell lines[1]. KPT-335 effectively hinders cell proliferation, prevents colony formation, and triggers cell apoptosis at doses that are biologically significant. It also leads to a decrease in XPO1 protein levels alongside an increase in XPO1 mRNA levels. Additionally, treatment with KPT-335 elevates the expression and nuclear presence of the tumor suppressor proteins p53 and p21[3]. Prophylactic and therapeutic use of verdinexor offers protection to mice from influenza virus strains A/California/04/09 and A/Philippines/2/82-X79, lowering lung viral counts and inflammatory cytokine levels while showing minimal toxicity[1]. The inhibition of XPO1 by KPT-335 also curtails cyst growth in vivo in the Pkd1 mutant mouse model Pkd1v/v[4].
Verdinexor 动物研究
Dose
Mice[3]: min = 10 mg/kg (p.o.), max = 50 mg/kg (p.o.); 5 mg/kg(i.v.)
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