YM155 is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM.
YM155 completely inhibits the tumor growth of PC-3 s.c. xenografted prostate tumors at doses of 3 and 10 mg/kg, without body weight loss and blood cell count decrease. Pharmacokinetic analysis shows that YM155 is highly distributed to tumor tissue. Moreover, YM155 shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts. The combination therapy with YM155 and -radiation shows great antitumor activity against H460 or Calu6 xenografts in nude mice.