Table 1.
Pharmacodynamic and antitumor response optimization for EMD1214063.
Treatment group | pY1234/1235MET/MET at relevant time point (%)a |
No. of animals exhibiting given antitumor responseb | |||
---|---|---|---|---|---|
PD | SD | PR | Total | ||
vehicle (BID) | 101.9 ± 48.6 | 8 | 0 | 0 | 8 |
3.125 mg/kg BID | 46.7 ± 10.9 | 5 | 1 | 4 | 10 |
12.5 mg/kg BID | 3.8 ± 3.9 | 0 | 3 | 7 | 10 |
50 mg/kg BID | 0.4 ± 0.1 | 0 | 1 | 9 | 10 |
100 mg/kg QD | 1.0 ± 0.5 | 0 | 0 | 10 | 10 |
Mean pY1234/1235MET/MET values (± standard deviation) for the time point at which next dose was scheduled to be administered in the given dosage regimen (12 h for all groups except 100 mg/kg QD, for which the response at 24 h is shown). For pharmacodynamic data, n = 6 animals per group.
No.: number; PD: progressive disease; SD: stable disease; PR: partial response. Antitumor responses were designated according to RECIST criteria, comparing tumor volumes for each animal on the day prior to administration of the first dose vs. last day of tumor measurement (days 16 vs. 48, respectively): PD: ≥ 20% tumor volume increase; PR: ≥ 30% reduction in tumor volume; SD: tumor volume change between −30% and +20%.