Table 4.

R547 exposures for efficacy

A. R547 exposures for efficacy in established tumor models
Tumor modelDose (mg/kg)Dosing route and scheduleCmax* (ng/mL)AUC/wk* (ng hr/mL)TGI (%)
HCT116 (human)30I.v. 1 × week27,00018,80091
HCT116 (human)40Oral daily86919,53791
MTLn3 (rat)15I.v. 1 × week13,10017,30089
MTLn3 (rat)80Oral 1 × week47412,00092
B. AUC vs Cmax exposures in MTLn3 rat model with q7d i.v. dosing
Dose (mg/kg)
Cmax* (ng/mL)
AUC/wk* (ng hr/mL)
TGI (%)
3.756,8402,260No efficacy
7.510,9005,730No efficacy
1513,10017,30089
3070,10056,70090
  • * Values calculated from end of efficacy study pharmacokinetic samples (n = 3).

  • 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.