From Proteopedia
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| Tyrosine Kinase Inhibitor Pharmacokinetics
|
|
| VEGFR & KIT Inhibitors
| EGFR Inhibitors
| BCR-Abl Inhibitor
|
| Parameter
| Sunitinib
(Sutent)
| Sorafenib
(Nexavar)
| Erlotinib
(Tarceva)
| Gefitinib
(Iressa)
| Lapatinib
(Tykerb)
| Imatinib
(Gleevec)
| Nilotinib
(Tasigna)
| Dasatinib
(Sprycel)
|
| Tmax (hr)
| 8
| 8.3
| 2.0
| 5.4
| 4
| 3.7
| 3.0
| 1.0
|
| Cmax (ng/ml)
| 24.6
| 460
| 69.6
| 130
| 115
| 2070
| 411
| 124
|
| Bioavailability (%)
| Variable
| 29-49
| 99
| 59
| Variable
| 98
| 30
| 20
|
| Protein Binding (%)
| 95
| 99
| 93
| 90
| 99
| 95
| 98
| 96
|
| T1/2 (hr)
| 83
| 29
| 9.4
| 26.9
| 9.6
| 26.6
| 16.0
| 3.3
|
| AUC (ng/ml/hr)
| 1921
| 11040
| 20577
| 3850
| 1429
| 4760
| 10052
| 461
|
| Dosage (mg)
| 50
| 50
| 150
| 250
| 100
| 400
| 200
| 200
|
| Metabolism
| Hepatic (CYP3A4)
| Hepatic (CYP3A4)
| Hepatic (CYP3A4)
| Hepatic (CYP3A4)
| Hepatic (CYP3A4)
| Hepatic (CYP3A4)
| Hepatic (CYP3A4)
| Hepatic (CYP3A4)
|
For Pharmacokinetic Data References, see: References
|
