Variable | Unit | Radioactivity | [^{14}C]Deferasirox: Plasma^{a} | Deferasirox (Steady State): Plasma | Complex (Steady State): Plasma | |
---|---|---|---|---|---|---|

Blood | Plasma | |||||

t_{max} (median) | h | 6 | 4 | 6 | 6 | 6 |

C_{max} | μmol/l | 20.2 ± 10.6 | 32.7 ± 18.4 | 30.6 ± 15.7 | 46.5 ± 22.7 | 4.7 ± 3.0 |

AUC_{24 h} | μmol · h/l^{b},^{c} | 292 ± 138 | 477 ± 229 | 434 ± 196 | 688 ± 307 | 79 ± 50 |

% ^{14}C-AUC_{24 h plasma} | 61 ± 2 | (100) | 91 ± 6 | |||

% ^{14}C-AUC_{plasma} | 60 ± 9 | 87 ± 21 | 9.8 ± 5.2 | |||

AUC_{t} | μmol · h/l^{b} | 434 ± 217 | 753 ± 351 | |||

t (median) | h | 48 | 72 | (24) | (24) | (24) |

AUC | μmol · h/l^{b} | 459 ± 207 | 785 ± 355 | 710 ± 291^{d} | ||

% ^{14}C-AUC_{plasma} | 59 ± 4 | (100) | 91 ± 6 | |||

t_{½} | h | 12.2 ± 2.8 | 9.6 ± 4.0 | 11.0 ± 5.3 | 9.4 ± 3.6 | —^{e} |

Time interval (typical) | h | 12–48 | 12–48 | 8–24 | 8–24 | |

Accumulation factor^{f} | 1.60 ± 0.37 |

↵a [

^{14}C]Deferasirox includes iron-complexed deferasirox. Under the conditions of the analytical system the radiolabeled complex cannot be measured separately.↵b AUC

_{24 h}and AUCwere calculated using the linear trapezoidal rule. AUC_{t}_{t}_{–∞}was calculated as*C*_{t}·*t*_{1/2}/ln2.↵c AUC

_{24 h}= AUC_{ss}for (cold) deferasirox and complex.↵d Extrapolated from AUC

_{24 h}using extrapolation factor 1.70 (from total^{14}C).↵e Individual half-lives of 11 and 25 h were measured in two subjects.

↵f AUC

_{ss}/AUC_{24 h}of [^{14}C]deferasirox. Corrected for the complex included in [^{14}C]deferasirox the factor is 1.97 ± 0.57.