Table 1.

Pharmacodynamic and antitumor response optimization for EMD1214063

Treatment grouppY1234/1235MET/MET at relevant time point (%)aNumber of animals exhibiting given antitumor responseb
Vehicle (BID)101.9 ± 48.68008
3.125 mg/kg BID46.7 ± 10.951410
12.5 mg/kg BID3.8 ± 3.903710
50 mg/kg BID0.4 ± 0.101910
100 mg/kg QD1.0 ± 0.5001010
  • aMean pY1234/1235MET/MET values (± SD) for the time point at which next dose was scheduled to be administered in the given dosage regimen (12 hours for all groups except 100 mg/kg once daily, for which the response at 24 hours is shown). For pharmacodynamic data, n = 6 animals per group.

  • bPD, 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 versus 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%.