Tyrosine Kinase Inhibitor Pharmacokinetics

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Revision as of 15:47, 9 December 2010

Tyrosine Kinase Inhibitor Pharmacokinetics
VEGFR & KIT Inhibitors EGFR Inhibitors PDGFR Inhibitor
Parameter Sunitinib
(Sutent)
Sorafenib
(Nexavar)
Erlotinib
(Tarceva)
Gefitinib
(Iressa)
Lapatinib
(Tykerb)
Imatinib
(Gleevec)
Tmax (hr) 8 8.3 2.0 5.4 4 Imatinib
(Gleevec)
Cmax (ng/ml) 24.6 460 69.6 130 115 Imatinib
(Gleevec)
Bioavailability (%) Variable 29-49 99 59 Variable Imatinib
(Gleevec)
Protein Binding (%) 95 99 93 90 99 Imatinib
(Gleevec)
T1/2 (hr) 83 29 9.4 26.9 9.6 Imatinib
(Gleevec)
AUC (ng/ml/hr) 1921 11040 20577 3850 1429 Imatinib
(Gleevec)
Dosage (mg) 50 50 150 250 100 Imatinib
(Gleevec)
Metabolism Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic - (CYP3A4) Hepatic - (CYP3A4) Hepatic - (CYP3A4) Imatinib
(Gleevec)

For references see: References

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David Canner

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