Table 2.

Pharmacokinetic, pharmacodynamic, and response data for 3 patients with colorectal cancer given [14C]oxaliplatin (Ox) as a microdose (Micro) or therapeutic dose (Thera) as part of the FOLFOX chemotherapy regimen.

2-Hour peakAUC serumOxaliplatin–DNA level: adducts/108 ntAUC: Adducts/Repair: adducts/108 nt per hourChemotherapy
serum oxaliplatin:oxaliplatin:In vivoIn vitro108 ntIn vivoIn vitroresponse after
Pt#Doseng/mL (Cmax)ng/mL per hour4 Hours24 Hours24 Hoursper hour3–4 cyclesa
1Micro12.468.473.0681.24248.83−0.091PR (−28%)
Thera1,1759,732217.8345.811,453+6.396
2Micro15.780.025.9632.824102.0−0.157PR (−72%)
Thera1,73610,5191,047617.831,228−21.48
3Micro11.586.363.7272.4604.88872.58−0.063+0.059PR (−41%)
Thera1,79218,215548.2649.1465.424,221+5.045−4.143
4Micro13.4108.92.1401.4001.47242.34−0.037−0.033Not evaluable
Thera1,14211,313287.1238.8258.09,872−2.412−1.453
5Micro8.666.062.7191.5361.93850.73−0.059−0.039PR (−41%)
Thera973.97,550172.8286.3121.99,568+5.475−2.544
6Micro14.3114.82.5892.0951.07156.51−0.025−0.076PD (+9%)
Thera1,25415,725315.2200.0305.710.513−5.760−0.476
  • Note: Response was determined according to RECIST criteria as either partial response (PR) or one almost complete response (CR) or progressive disease (PD).

  • Abbreviation: Pt#, patient number.

  • aNumbers represent percent tumor shrinkage after last cycle.