Tyrosine Kinase Inhibitor Pharmacokinetics
From Proteopedia
(Difference between revisions)
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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=" | + | ! 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=" | + | ! colspan="3" align="center"| BCR-Abl Inhibitor |
|- | |- | ||
! Parameter | ! Parameter | ||
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! [[Imatinib]]<br/>(Gleevec) | ! [[Imatinib]]<br/>(Gleevec) | ||
! [[Nilotinib]]<br/>(Tasigna) | ! [[Nilotinib]]<br/>(Tasigna) | ||
| + | ! [[Dasatinib]]<br/>(Sprycel) | ||
|- | |- | ||
! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr) | ! [[Pharmacokinetics#Tmax|T<sub>max</sub>]] (hr) | ||
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! 3.7 | ! 3.7 | ||
! 3.0 | ! 3.0 | ||
| + | ! 1.0 | ||
|- | |- | ||
! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml) | ! [[Pharmacokinetics#Cmax|C<sub>max</sub>]] (ng/ml) | ||
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! 2070 | ! 2070 | ||
! 411 | ! 411 | ||
| + | ! 124 | ||
|- | |- | ||
! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%) | ! [[Pharmacokinetics#Bioavailability_.28F.29|Bioavailability]] (%) | ||
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! 98 | ! 98 | ||
! 30 | ! 30 | ||
| + | ! 20 | ||
|- | |- | ||
! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%) | ! [[Pharmacokinetics#Protein_Binding|Protein Binding]] (%) | ||
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! 95 | ! 95 | ||
! 98 | ! 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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! 26.6 | ! 26.6 | ||
! 16.0 | ! 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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! 4760 | ! 4760 | ||
! 10052 | ! 10052 | ||
| + | ! 461 | ||
|- | |- | ||
! Dosage (mg) | ! Dosage (mg) | ||
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! 100 | ! 100 | ||
! 400 | ! 400 | ||
| + | ! 200 | ||
! 200 | ! 200 | ||
|- | |- | ||
! Metabolism | ! Metabolism | ||
| + | ! Hepatic (CYP3A4) | ||
! Hepatic (CYP3A4) | ! Hepatic (CYP3A4) | ||
! Hepatic (CYP3A4) | ! Hepatic (CYP3A4) | ||
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
