Trastuzumab

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spinqualitylabelsall models Tastuzumab, better known as Herceptin, (3bdy) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Better Known as: Herceptin

• Marketed By: Genentech
  
• Major Indication: Breast Cancer
  
• Drug Class: Human Epidermal Growth Factor Receptor 2 (HER2) Inhibitor
• Date of FDA Approval (Discontinued): 1998 (2015)
  
• 2008 Sales: $4.75 Billion
• Importance: It is a very effective treatment against HER2-positive metastatic breast cancer compared to other cancer therapies. Controversial due to its cost of nearly $100,000 per year. Is often pointed to as an example of the benefits of personalized medicine in which a patent's genetic profile is used to optimize their medication regimen.
• The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information

Mechanism of Action

Human Epidermal Growth Factor Receptor 2 (HER2)

Pharmacokinetics

EGFR Inhibitor Pharmacokinetics[1][2]
Parameter	Trastuzumab
Tmax (hr)	1.7
Cmax (ng/ml)	203000
Bioavailability (%)	54
T1/2 (days)	27
AUC (ug/ml/hr)	45036
Clearance (L/h)	.009
Dosage (mg)	250
Metabolism	Unknown

References

1. ↑ Leyland-Jones B, Gelmon K, Ayoub JP, Arnold A, Verma S, Dias R, Ghahramani P. Pharmacokinetics, safety, and efficacy of trastuzumab administered every three weeks in combination with paclitaxel. J Clin Oncol. 2003 Nov 1;21(21):3965-71. Epub 2003 Sep 24. PMID:14507946 doi:10.1200/JCO.2003.12.109
2. ↑ B. Leyland-Jones, et al. Pharmacologic insights into the future of trastuzumab. Annals of Oncology 12 (Suppl. I): S43-S47, 2001.