Table 3.

Selected mean (SD) pharmacokinetic parameters for total antibody and unconjugated MMAE after DLYE5953A treatment at cycle 1.

Total antibodyNumber of patientsaCmax (μg/mL)AUC0-inf (day*μg/mL)t1/2 (day)Vss (mL/kg)CL (mL/day/kg)
Cohorts:
 0.2 mg/kg33.4513.67.0512616.6
(1.14)(6.2)(1.61)(39)(6.1)
 0.4 mg/kg37.7429.88.3810913.6
(0.62)(3.6)(1.89)(13.9)(1.8)
 0.8 mg/kg316.189.713.312910.1
(4.6)(37.1)(1.2)(41)(4.0)
 1.6 mg/kg436.91414.9771.612.0
(8.9)(37)(1.94)(27.3)(2.5)
 2.4 mg/kg744.12197.6090.511.9
(11.5)(69)(2.709)(20.4)(3.3)
 2.4 mg/kg2247.02587.0288.010.0
 MBC(9.7)(77)(2.31)(24.4)(2.7)
 2.4 mg/kg2446.42537.2787.410.9
 NSCLC(7.6)(101)(2.38)(20.9)(4.4)
Unconjugated MMAENumber of patientsaCmax (ng/mL)AUC0-inf (day*ng/mL)tmax (day)
Cohorts:
 0.2 mg/kg30.4613.181.64
(0.057)(0.61)(0.57)
 0.4 mg/kg30.7287.131.65
(0.161)(NA)(0.57)
 0.8 mg/kg31.6913.42.01
(1.05)(11.7)(0.05)
 1.6 mg/kg46.1766.65.43
(3.85)(35.6)(6.95)
 2.4 mg/kg76.0753.13.01
(2.26)(27)(2.62)
 2.4 mg/kg144.0834.93.10
 MBC(2.08)(18.2)(3.46)
 2.4 mg/kg104.8536.52.71
 NSCLC(2.44)(16.8)(2.23)
  • Abbreviations: AUC0-inf, area under the concentration−time curve from time zero extrapolated to infinite time; CL, clearance; Cmax, maximum observed plasma concentration; Vss, volume of distribution at steady state; t1/2, terminal half-life; tmax, time to reach maximum concentration.

  • aNumber of patients with at least one pharmacokinetic parameter estimated.