Table 3.

In vivo efficacy with oral and i.v. dosing of R547 in established human tumor models

Tumor model (source)TGI (%),* 40 mg/kg once daily oral dosingFinal mean tumor volume ± SD (mm3)
TGI (%),* 40 mg/kg once weekly i.v. dosingFinal mean tumor volume ± SD (mm3)
VehicleR547VehicleR547
HCT 116 (colon)911,658 ± 334.09229.8 ± 72.0881,292.24 ± 426.01240.50 ± 98.02
H460a (lung)801,053.0 ± 545.6268.78 ± 118.01611,674.43 ± 693.15738.12 ± 375.92
MDA-MB-435 (breast)79509.38 ± 175.21220.23 ± 39.2578509.38 ± 175229.02 ± 50.63
DU145 (prostate)85623.11 ± 139.27184.34 ± 68.4195365.76 ± 223.85122.67 ± 49.17
A549 (lung)98920.57 ± 221.02133.66 ± 55.4992920.57 ± 221.02180.82 ± 59.38
LOX (melanoma)992,568.4 ± 1,211117.39 ± 37.70NDNDND
  • Abbreviation: ND, not determined.

  • * Percentage change in tumor volume is calculated using the following formula: [(TT0) / T0] × 100, where ‘T’ represents mean tumor volume of the treated group at a particular day and ‘T0’ represents mean tumor volume of the same treated group at initiation of treatment.

  • P < 0.01.