Erlotinib
From Proteopedia
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===Better Known as: Tarceva=== | ===Better Known as: Tarceva=== | ||
* Marketed By: Genentech, OSI Pharmaceutials, & Roche | * Marketed By: Genentech, OSI Pharmaceutials, & Roche | ||
Revision as of 12:54, 28 November 2010
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Better Known as: Tarceva
- Marketed By: Genentech, OSI Pharmaceutials, & Roche
- Major Indication: Pancreatic & Small Cel Lung Cancer
- Drug Class: EGFR Inhibitor
- Date of FDA Approval (Expiration): 2005 (2020)
- 2009 Sales: $1.2 Billion
- Why You Should Care: It is one of the best selling and most effective treatments for several types of cancer.
- The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information
Pharmacokinetics
| EGFR Inhibitor Pharmacokinetics Comparison at Equivalent Dosages [1][2] | |||||
|---|---|---|---|---|---|
| Parameter | Erlotinib (Tarceva) | Gefitinib (Iressa) | |||
| Tmax (hr) | 2.0 | 5.4 | |||
| Cmax (ng/ml) | 69.6 | 130 | |||
| Bioavailability (%) | 99 | 60 | |||
| Protein Binding (%) | 93 | 90 | |||
| T1/2 (hr) | 9.4 | 26.9 | |||
| AUC (ng/ml/hr) | 20577 | 3850 | |||
| IC50 (nM) | 2 | 23 | |||
| Typical Dosage (mg) | 150 | 250 | |||
| Metabolism | Hepatic - (CYP3A4, CYP3A5, CYP2D6, CYP1A1) | Hepatic - (CYP3A4, CYP3A5, CYP2D6, CYP1A1, CYP1A2) | |||
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
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