Gefitinib
From Proteopedia
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* The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information | * The following is a list of Pharmacokinetic Parameters. See: [[Pharmaceutical Drugs]] for more information | ||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
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{| class="wikitable" border="1" width="40%" style="text-align:center" | {| class="wikitable" border="1" width="40%" style="text-align:center" | ||
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! 2.0 | ! 2.0 | ||
! 5.4 | ! 5.4 | ||
| - | ! | + | ! 4 |
|- | |- | ||
! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml) | ! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml) | ||
! 69.6 | ! 69.6 | ||
! 130 | ! 130 | ||
| - | ! | + | ! 115 |
|- | |- | ||
! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%) | ! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%) | ||
! 99 | ! 99 | ||
! 59 | ! 59 | ||
| - | ! | + | ! Lapatinib (Tykerb) |
|- | |- | ||
! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%) | ! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%) | ||
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! 9.4 | ! 9.4 | ||
! 26.9 | ! 26.9 | ||
| - | ! | + | ! 9.6 |
|- | |- | ||
! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ||
! 20577 | ! 20577 | ||
! 3850 | ! 3850 | ||
| - | ! | + | ! 1429 |
|- | |- | ||
! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM) | ! [[Pharmaceutical_Drugs#Inhibitory_Concentration_.28IC50.29|IC<sub>50</sub>]] (nM) | ||
! 2 | ! 2 | ||
! 23 | ! 23 | ||
| - | ! | + | ! |
|- | |- | ||
! Typical Dosage (mg) | ! Typical Dosage (mg) | ||
! 150 | ! 150 | ||
! 250 | ! 250 | ||
| - | ! | + | ! 100 |
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! Metabolism | ! Metabolism | ||
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! Hepatic (CYP3A4) | ! Hepatic (CYP3A4) | ||
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===References=== | ===References=== | ||
Revision as of 08:38, 6 December 2010
|
Better Known as: Iressa
- Marketed By: AstraZeneca & Teva
- Major Indication: Pancreatic & Small Cel Lung Cancer
- Drug Class: EGFR Inhibitor
- Date of FDA Approval (Expiration): 2003 (2013)
- 2009 Sales: $268 Million
- Importance: It is the first selective inhibitor of Epidermal Growth Factor Receptors approved by the FDA
- The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information
Pharmacokinetics
| EGFR Inhibitor Pharmacokinetics Comparison at Equivalent Dosages [1][2][3] | |||
|---|---|---|---|
| Parameter | Erlotinib (Tarceva) | Gefitinib (Iressa) | Lapatinib (Tykerb) |
| Tmax (hr) | 2.0 | 5.4 | 4 |
| Cmax (ng/ml) | 69.6 | 130 | 115 |
| Bioavailability (%) | 99 | 59 | Lapatinib (Tykerb) |
| Protein Binding (%) | 93 | 90 | 99 |
| T1/2 (hr) | 9.4 | 26.9 | 9.6 |
| AUC (ng/ml/hr) | 20577 | 3850 | 1429 |
| IC50 (nM) | 2 | 23 | |
| Typical Dosage (mg) | 150 | 250 | 100 |
| Metabolism | Hepatic - (CYP3A4, CYP3A5, CYP2D6, CYP1A1) | Hepatic - (CYP3A4, CYP3A5, CYP2D6, CYP1A1, CYP1A2) | Hepatic (CYP3A4) |
References
- ↑ Hamilton M, Wolf JL, Rusk J, Beard SE, Clark GM, Witt K, Cagnoni PJ. Effects of smoking on the pharmacokinetics of erlotinib. Clin Cancer Res. 2006 Apr 1;12(7 Pt 1):2166-71. PMID:16609030 doi:10.1158/1078-0432.CCR-05-2235
- ↑ Bergman E, Forsell P, Persson EM, Knutson L, Dickinson P, Smith R, Swaisland H, Farmer MR, Cantarini MV, Lennernas H. Pharmacokinetics of gefitinib in humans: the influence of gastrointestinal factors. Int J Pharm. 2007 Aug 16;341(1-2):134-42. Epub 2007 Apr 6. PMID:17482782 doi:10.1016/j.ijpharm.2007.04.002
- ↑ D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.
