Lapatinib

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

Lapatinib, also known as Tykerb

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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 (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

  1. ↑ 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
  2. ↑ 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
  3. ↑ D. Smith et al. Br J Clin Pharmacol. 2009 April; 67(4): 421–426.


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