Table 1.

In vivo activity of AZD1152 against a range of human tumor xenograft models

Tumor modelTumor originDose (mg/kg/d)Route (duration)Inhibition of tumor volume (%)
MaximumEnd of study
SW620Human colon150S.c. mini-pump (48 h, days 7-9)87* (day 23)87* (day 23)
25S.c. mini-pump (48 h, days 7-9)65 (day 14)49 (day 23)
10S.c. mini-pump (48 h, days 7-9)55 (day 10)28 (day 23)
25I.p. bolus daily (4 d, days 6-9)65 (day 13)54* (day 24)
25I.v. bolus daily (3 d, days 6-8)91* (day 13)47 (day 24)
Colo205Human colon150S.c. mini-pump (48 h, days 5-7)>100* (day 18)94* (day 21)
HCT116Human colon150S.c. mini-pump (48 h, days 11-13)93* (day 18)74* (day 25)
A549Human lung150S.c. mini-pump (48 h, days 13-15)79 (day 26)69 (day 29)
25S.c. mini-pump (48 h, days 13-15)74 (day 15)36 (day 29)
Calu-6Human lung150S.c. mini-pump (48 h, days 20-22)67 (day 29)55* (day 41)
HL-60§Human leukemia150S.c. mini-pump (48 h, days 16-18)>100* (day 18)>100* (day 35)
  • NOTE: Human tumor xenografts were established in the flank of male Swiss athymic mice (8-12 wks of age). Mice were randomized into treatment groups when tumors reached a mean volume of 0.2 to 0.5 cm3 and then treated with a continuous infusion of AZD1152 or vehicle (0.3 mol/L Tris buffer) via a s.c. implanted mini-pump or as a once-daily i.p or i.v bolus. Percentage tumor growth inhibition was calculated as the difference between the change in control and AZD1152-treated tumor volumes during and following the treatment period. Statistical significance was calculated using a one-tailed t test. P value of <0.05 was considered to be statistically significant.

  • * P < 0.0005.

  • P < 0.005.

  • P < 0.05.

  • § No palpable or measurable tumors in 8 of 11 animals following treatment with AZD1152.