Tyrosine Kinase Inhibitor Pharmacokinetics

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{| class="wikitable" border="0" width="100%" style="text-align:center"
{| class="wikitable" border="0" width="100%" style="text-align:center"
|-
|-
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! colspan="7" align="center"| Tyrosine Kinase Inhibitor [[Pharmacokinetics]]
+
! colspan="9" align="center"| Tyrosine Kinase Inhibitor [[Pharmacokinetics]]
|-
|-
! colspan="1" align="center"|
! colspan="1" align="center"|
! colspan="2" align="center"| [[VEGFR]] & KIT Inhibitors
! colspan="2" align="center"| [[VEGFR]] & KIT Inhibitors
! colspan="3" align="center"| [[EGFR]] Inhibitors
! colspan="3" align="center"| [[EGFR]] Inhibitors
-
! colspan="1" align="center"| PDGFR Inhibitor
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! colspan="3" align="center"| BCR-Abl Inhibitor
|-
|-
! Parameter
! Parameter
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! [[Lapatinib]]<br/>(Tykerb)
! [[Lapatinib]]<br/>(Tykerb)
! [[Imatinib]]<br/>(Gleevec)
! [[Imatinib]]<br/>(Gleevec)
 +
! [[Nilotinib]]<br/>(Tasigna)
 +
! [[Dasatinib]]<br/>(Sprycel)
|-
|-
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
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! 4
! 4
! 3.7
! 3.7
 +
! 3.0
 +
! 1.0
|-
|-
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
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! 115
! 115
! 2070
! 2070
 +
! 411
 +
! 124
|-
|-
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
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! Variable
! Variable
! 98
! 98
 +
! 30
 +
! 20
|-
|-
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
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! 99
! 99
! 95
! 95
 +
! 98
 +
! 96
|-
|-
! [[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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! 9.6
! 9.6
! 26.6
! 26.6
 +
! 16.0
 +
! 3.3
|-
|-
! [[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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! 1429
! 1429
! 4760
! 4760
 +
! 10052
 +
! 461
|-
|-
! Dosage (mg)
! Dosage (mg)
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! 100
! 100
! 400
! 400
 +
! 200
 +
! 200
|-
|-
! Metabolism
! Metabolism
 +
! Hepatic (CYP3A4)
 +
! Hepatic (CYP3A4)
! Hepatic (CYP3A4)
! Hepatic (CYP3A4)
! Hepatic (CYP3A4)
! Hepatic (CYP3A4)
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! Hepatic (CYP3A4)
! Hepatic (CYP3A4)
|}
|}
-
For references, see: [[Treatments:TYKI References|References]]
+
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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