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| | ===Pharmacokinetics=== | | ===Pharmacokinetics=== |
| - | | + | <table style="background: cellspacing="0px" align="" cellpadding="0px" width="50%"> |
| - | {| class="wikitable" border="1" width="40%" style="text-align:center"
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| + | <td style="width:auto; vertical-align:top;border-width:0px; border-style:inset"> |
| - | ! colspan="6" align="center"| VEGFR 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>
| + | <div style="overflow:auto; height:100%; width: 100%"> |
| - | |-
| + | {{:Tyrosine Kinase Inhibitor Pharmacokinetics}} |
| - | ! Parameter
| + | </div> |
| - | ! [[Sunitinib]] (Sutent)
| + | </td> |
| - | ! [[Sorafenib]] (Nexavar)
| + | </tr> |
| - | |-
| + | </table> |
| - | ! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr)
| + | |
| - | ! 8
| + | |
| - | ! 8.3
| + | |
| - | |-
| + | |
| - | ! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml)
| + | |
| - | ! 24.6
| + | |
| - | ! 460
| + | |
| - | |-
| + | |
| - | ! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%)
| + | |
| - | ! Variable
| + | |
| - | ! 29-49
| + | |
| - | |-
| + | |
| - | ! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%)
| + | |
| - | ! 95
| + | |
| - | ! 99
| + | |
| - | |-
| + | |
| - | ! [[Pharmacokinetics#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr)
| + | |
| - | ! 83
| + | |
| - | ! 29
| + | |
| - | |-
| + | |
| - | ! [[Pharmacokinetics#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr)
| + | |
| - | ! 1921
| + | |
| - | ! 11040
| + | |
| - | |-
| + | |
| - | ! Dosage (mg)
| + | |
| - | ! 50
| + | |
| - | ! 50
| + | |
| - | |-
| + | |
| - | ! Metabolism
| + | |
| - | ! Hepatic (CYP3A4)
| + | |
| - | ! Hepatic (CYP3A4)
| + | |
| - | |}
| + | |
Revision as of 13:29, 9 December 2010
Pharmacokinetics
| 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
|
