Table 1.

Efficacy of BI 885578 in colorectal cancer xenograft models

ModelIGF2 (TPM)IGF2 ClassificationKRASPI3K p110αBI 885578 TGI (%)P (vs. control)Treatment duration (days)
CL-143,223HighNDWT920.000926
LS10431,649HighWTND540.004122
GEO683HighG12AWT69–750.0003–0.001217–22
C2BBe1410HighWTWT720.000922
LoVo5LowG13DWT100.3121
SW481LowWTG914R40.402418
HCT-151LowG13DE545K/D549N320.064117
  • NOTE: Tumor-bearing mice (7/group) were treated with BI 885578 (40 mg/kg) or vehicle control. IGF2 gene expression and mutation status of KRAS and PI3K p110α for the corresponding cell line grown in vitro are indicated for each xenograft model. The TGI and corresponding P values (BI 885578 vs. control group) were calculated on the last day of treatment. The GEO model was tested in five independent experiments and the range of TGI values, P values and treatment durations is indicated. Tumor models are sorted according to IGF2 expression. IGF2high = TPM ≥ 72. IGF2low = TPM < 72.

  • Abbreviations: ND, not determined; WT, wild-type.