Gefitinib: Difference between revisions
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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 | ||
===Mechanism of Action=== | ===Mechanism of Action=== | ||
[[EGFR|Epidermal Growth Factor Receptors]] are overexpressed | [[EGFR|Epidermal Growth Factor Receptors]] are overexpressed in many types of human [[Cancer|carcinomas]] including lung, pancreatic, and breast cancer. This overexpression leads to excessive activation of the anti-apoptotic [[Ras]] signalling cascade. | ||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
Revision as of 10:03, 7 December 2010
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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
Mechanism of Action
Epidermal Growth Factor Receptors are overexpressed in many types of human carcinomas including lung, pancreatic, and breast cancer. This overexpression leads to excessive activation of the anti-apoptotic Ras signalling cascade.
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 | Variable |
| Protein Binding (%) | 93 | 90 | 99 |
| T1/2 (hr) | 9.4 | 26.9 | 9.6 |
| AUC (ng/ml/hr) | 20577 | 3850 | 1429 |
| Typical Dosage (mg) | 150 | 250 | 100 |
| Metabolism | Hepatic - (CYP3A4) | Hepatic - (CYP3A4) | 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.