In vitro binding of [14C]deferasirox and its iron complex [14C]Fe-[ICL670]2 to isolated human plasma proteins Given numbers are mean ± S.D. of triplicate determinations. Used plasma protein concentrations are in the range of concentrations found in plasma of healthy subjects with the exception of 1 mg/ml HSA.
Protein and Used Concentration | Concentration | Unbound Fraction in Protein Solution | ||
|---|---|---|---|---|
| Deferasirox | Fe-[ICL670]2a | |||
| μg/ml | % | |||
| HSA, 40 mg/ml | 4 | 1.3 ± 0.1 | 0.4 ± <0.1 | |
| 20 | 1.1 ± <0.1 | 0.3 ± <0.1 | ||
| 80 | 1.3 ± <0.1 | 0.5 ± <0.1 | ||
| HSA, 1 mg/ml | 4 | 22 ± 0.3 | 11 ± 0.4 | |
| 20 | 28 ± 0.2 | 22 ± 0.3 | ||
| 80 | 52 ± 0.9 | 53 ± 0.2 | ||
| α1-Acid glycoprotein, 1 mg/ml | 20 | 58 ± 2 | 91 ± 2 | |
| γ-Globulin, 12 mg/ml | 20 | 67 ± 0.4 | 70 ± 2 | |
| VLDL, 1.3 mg/ml | 20 | 16 ± 0.5 | 85 ± 2 | |
| LDL, 3.6 mg/ml | 20 | 11 ± 0.2 | 64 ± 1 | |
| HDL, 3.9 mg/ml | 20 | 6.8 ± 0.2 | 27 ± 0.3 | |
VLDL, very low density lipoprotein; LDL, low density lipoprotein; HDL, high density lipoprotein
↵ a In incubations with low concentrations of [14C]Fe-[ICL670]2, significant decay of the iron complex occurs during incubation; see under Materials and Methods, Control Experiments