Lapatinib
From Proteopedia
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===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
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! colspan="4" align="center"| EGFR Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]] Comparison at Equivalent Dosages <ref>PMID:16609030</ref><ref>PMID:17482782</ref><ref>D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.</ref> | ! colspan="4" align="center"| EGFR Inhibitor [[Pharmaceutical_Drugs#Pharmacokinetics_Translated|Pharmacokinetics]] Comparison at Equivalent Dosages <ref>PMID:16609030</ref><ref>PMID:17482782</ref><ref>D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.</ref> | ||
Revision as of 08:32, 7 December 2010
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Better Known as: Tykerb
- Marketed By: GlaxoSmithKline
- Major Indication: Breast Cancer
- Drug Class: EGFR Inhibitor
- Date of FDA Approval (Expiration): 2007 (2017)
- 2009 Sales (Projected Peak): $150 Million ($4.5 Billion)[1]
- Importance: It is one of the newest treatments for cancer. Complaints over the high cost ($22,000) for a treatment course which only prolongs survival in breast cancer patients by less than 2 months.
- The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information
Pharmacokinetics
| EGFR Inhibitor Pharmacokinetics Comparison at Equivalent Dosages [2][3][4] | |||
|---|---|---|---|
| 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
- ↑ http://money.cnn.com/2006/06/03/news/companies/glaxo_breastcancer/index.htm
- ↑ 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.
