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Lapatinib
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| + | <applet load="" size="480" color="" frame="true" spin="on" Scene ="" align="right" caption="Lapatinib, also known as Tykerb"/> | ||
| + | ===Better Known as: Tykerb=== | ||
| + | * Marketed By: GlaxoSmithKline | ||
| + | * Major Indication: Breast [[Cancer]] | ||
| + | * Drug Class: [[EGFR]] Inhibitor | ||
| + | * Date of FDA Approval (Expiration): 2007 (2020) | ||
| + | * 2009 Sales: $1.2 Billion | ||
| + | * Importance: 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=== | ||
| + | {| class="wikitable" border="1" width="40%" style="text-align:center" | ||
| + | |- | ||
| + | ! 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> | ||
| + | |- | ||
| + | ! Parameter | ||
| + | ! [[Erlotinib]] (Tarceva) | ||
| + | ! [[Gefitinib]] (Iressa) | ||
| + | ! Lapatinib (Tykerb) | ||
| + | |- | ||
| + | ! [[Pharmaceutical_Drugs#Tmax|T<sub>max</sub>]] (hr) | ||
| + | ! 2.0 | ||
| + | ! 5.4 | ||
| + | ! 4 | ||
| + | |- | ||
| + | ! [[Pharmaceutical_Drugs#Cmax|C<sub>max</sub>]] (ng/ml) | ||
| + | ! 69.6 | ||
| + | ! 130 | ||
| + | ! 115 | ||
| + | |- | ||
| + | ! [[Pharmaceutical_Drugs#Bioavailability_.28F.29|Bioavailability]] (%) | ||
| + | ! 99 | ||
| + | ! 59 | ||
| + | ! Variable | ||
| + | |- | ||
| + | ! [[Pharmaceutical_Drugs#Protein_Binding|Protein Binding]] (%) | ||
| + | ! 93 | ||
| + | ! 90 | ||
| + | ! 99 | ||
| + | |- | ||
| + | ! [[Pharmaceutical_Drugs#Half_Life_.28T1.2F2.29|T<sub>1/2</sub>]] (hr) | ||
| + | ! 9.4 | ||
| + | ! 26.9 | ||
| + | ! 9.6 | ||
| + | |- | ||
| + | ! [[Pharmaceutical_Drugs#Area_Under_the_Curve_.28AUC.29|AUC]] (ng/ml/hr) | ||
| + | ! 20577 | ||
| + | ! 3850 | ||
| + | ! 1429 | ||
| + | |- | ||
| + | ! Typical Dosage (mg) | ||
| + | ! 150 | ||
| + | ! 250 | ||
| + | ! 100 | ||
| + | |- | ||
| + | ! Metabolism | ||
| + | ! Hepatic - (CYP3A4, CYP3A5, CYP2D6, CYP1A1) | ||
| + | ! Hepatic - (CYP3A4, CYP3A5, CYP2D6, CYP1A1, CYP1A2) | ||
| + | ! Hepatic (CYP3A4) | ||
| + | |} | ||
| + | ===References=== | ||
| + | <references/> | ||
| + | __NOEDITSECTION__ | ||
| + | __NOTOC__ | ||
Revision as of 11:56, 6 December 2010
|
Better Known as: Tykerb
- Marketed By: GlaxoSmithKline
- Major Indication: Breast Cancer
- Drug Class: EGFR Inhibitor
- Date of FDA Approval (Expiration): 2007 (2020)
- 2009 Sales: $1.2 Billion
- Importance: 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][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, 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.
