Table 3.

Broad-spectrum antitumor activity of OSI-027

Cell lineTumor typePTEN/PIK3CA/KRAS/BRAF mutation statusOSI-027 dose, dailyTumor growth inhibition (%)Maximum regression (%)
MCF-7BreastPIK3CA mt65 mg/kg879
MDA-MB-468BreastPTEN null50 mg/kg9926
HCT-116ColonPIK3CA mt, KRAS mt65 mg/kg10018
NCI-H292Lungwt50 mg/kg618
NCI-H460LungPIK3CA mt, KRAS mt50 mg/kg840
DU145Prostatewt65 mg/kg580
RLLymphomawt65 mg/kg10027
FADUHNSCCwt50 mg/kg860

NOTE: OSI-027 was administered orally once daily at indicated dose for 14 days. The percentages of TGI and regression were calculated as described in Materials and Methods. n = 8 animals per group in all studies.

Abbreviation: HNSCC, head and neck squamous cell carcinomas.