Table 4.

Pharmacokinetic parameters for eribulin mesylate administered on day 1 of a 21-day cycle (noncompartmental model)

Pharmacokinetic parameters
Dose* (mg/m2)nCmax (μg/mL)AUC0-∞ (h μg/mL)t1/2(h)Vss(L/m2)Cmax/dose (μg/mL)AUC0-∝/dose (h μg/mL)CL (L/h/m2)
Mean (SD)%CVMean (SD)%CVMean (SD)%CVMean (SD)%CVMean (SD)%CVMean (SD)%CVMean (SD)%CV
0.25 (0.221)*10.0440.13835.253.30.1970.6241.60
0.5 (0.442)*40.063 (0.02)290.210 (0.05)2634.4 (6.78)2067.6 (25.24)370.142 (0.04)290.474 (0.12)262.22 (0.57)26
1 (0.884)*30.127 (0.04)310.486 (0.33)6845.9 (21.92)4886.7 (11.55)130.144 (0.04)310.550 (0.38)682.42 (1.38)57
2 (1.767)*70.369 (0.04)101.842 (0.85)4648.8 (22.07)4547.8 (10.14)210.209 (0.02)101.042 (0.48)461.16 (0.54)47
2.8 (2.474)*30.340 (0.13)391.412 (0.63)4442.3 (6.75)1687.4 (49.32)560.138 (0.05)390.571 (0.25)442.12 (1.25)59
4 (3.535)*30.528 (0.18)342.334 (0.91)3966.0 (21.50)33114.2 (16.36)140.149 (0.05)340.660 (0.26)391.70 (0.75)44
All doses21n/an/an/an/a46.5 (18.68)4072.5 (31.17)430.168 (0.05)280.722 (0.40)551.78 (0.89)50
  • Abbreviations: AUC0-∞, area under the concentration-time curve; Cmax, maximal plasma concentration; CV, coefficient of variation; n/a, not applicable; t1/2, elimination half-life; Vss, volume of distribution at steady state.

  • * Doses given are for the eribulin mesylate salt; doses in parentheses are the free base dose equivalents.

  • Normalized for each 1 mg/m2 of free base equivalent dose.