Lapatinib

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spinqualitylabelsall models Lapatinib, also known as Tykerb Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

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)
• 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 [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.