Table 5.

PK variables of XRP6258

Dose (mg/m2)No. patientsPK variables (data expressed as mean ± SD)
Cmax (μg/L)*AUC(0-48 h) (μg.h/L)*AUC (μg.h/L)t1/2λ3 (h)CL (L/h/m2)Vss (L/m2)
10375.8 ± 31.7203 ± 52361 ± 12850.7 ± 14.230.1 ± 11.21,623 ± 533
156287 ± 273392 ± 271745 ± 21555.2 ± 35.621.3 ± 6.01,266 ± 1,255
209222 ± 207373 ± 157766 ± 30695.6 ± 53.429.7 ± 12.12,637 ± 1,657
21§148747768741.030.4547
254535 ± 305642 ± 3201,038 ± 29981.9 ± 41.425.0 ± 5.61,985 ± 1,615
Overall2377.3 ± 45.527.3 ± 9.72,034 ± 1,495
  • * Noncompartmental analysis.

  • Individual modeling.

  • One patient treated at 25 mg/m2 was not evaluable for PK but was treated at 20 mg/m2 at the second cycle.

  • § One patient included in the 25 mg/m2 cohort was found to have a high BSA (2.53 m2); therefore, treatment was done with dose adjustment based on a restricted BSA of 2.1 m2, and subsequently, he only received a dose of 21 mg/m2.