Tyrosine Kinase Inhibitor Pharmacokinetics

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! colspan="6" align="center"| Tyrosine Kinase Inhibitor [[Pharmacokinetics]] <ref>D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.</ref><ref>R. Khosravan, et al. General Poster Session, Developmental Therapeutics: Cytotoxic Chemotherapy, J Clin Oncol 26: 2008 (May 20 suppl; abstr 2578)</ref><ref>PMID:16133532</ref><ref>PMID:20821331</ref><ref>PMID:20717111</ref><ref>PMID:16609030</ref><ref>PMID:17482782</ref><ref>D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.</ref>
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! colspan="9" align="center"| Tyrosine Kinase Inhibitor [[Pharmacokinetics]]
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|-
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! colspan="1" align="center"|
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! colspan="2" align="center"| [[VEGFR]] & KIT Inhibitors
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! colspan="3" align="center"| [[EGFR]] Inhibitors
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! colspan="3" align="center"| BCR-Abl Inhibitor
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! Parameter
! Parameter
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! [[Sunitinib]] (Sutent)
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! [[Sunitinib]]<br/>(Sutent)
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! [[Sorafenib]] (Nexavar)
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! [[Sorafenib]]<br/>(Nexavar)
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! [[Erlotinib]] <br/>(Tarceva)
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! [[Erlotinib]]<br/>(Tarceva)
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! [[Gefitinib]] <br/>(Iressa)
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! [[Gefitinib]]<br/>(Iressa)
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! [[Lapatinib]] <br/>(Tykerb)
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! [[Lapatinib]]<br/>(Tykerb)
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! [[Imatinib]]<br/>(Gleevec)
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! [[Nilotinib]]<br/>(Tasigna)
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! [[Dasatinib]]<br/>(Sprycel)
|-
|-
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
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! 5.4
! 5.4
! 4
! 4
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! 3.7
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! 3.0
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! 1.0
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|-
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
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! 130
! 130
! 115
! 115
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! 2070
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! 411
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! 124
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|-
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
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! 59
! 59
! Variable
! Variable
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! 98
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! 30
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! 20
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|-
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
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! 90
! 90
! 99
! 99
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! 95
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! 98
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! 96
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|-
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
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! 26.9
! 26.9
! 9.6
! 9.6
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! 26.6
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! 16.0
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! 3.3
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|-
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
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! 3850
! 3850
! 1429
! 1429
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! 4760
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! 10052
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! 461
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! Dosage (mg)
! Dosage (mg)
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! 250
! 250
! 100
! 100
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! 400
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! 200
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! 200
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! Metabolism
! Metabolism
! Hepatic (CYP3A4)
! Hepatic (CYP3A4)
! Hepatic (CYP3A4)
! Hepatic (CYP3A4)
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! Hepatic - (CYP3A4)
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! Hepatic (CYP3A4)
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! Hepatic - (CYP3A4)
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! Hepatic (CYP3A4)
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! Hepatic - (CYP3A4)
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! Hepatic (CYP3A4)
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! Hepatic (CYP3A4)
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! Hepatic (CYP3A4)
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! Hepatic (CYP3A4)
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For Pharmacokinetic Data References, see: [[Treatments:TYKI References|References]]

Current revision

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

Proteopedia Page Contributors and Editors (what is this?)

David Canner

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