Trastuzumab: Difference between revisions

Revision as of 16:52, 8 December 2010

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

EGFR Inhibitor Pharmacokinetics^[1]
Parameter	Trastuzumab
T_max (hr)	1.7
C_max (ng/ml)	203000
Bioavailability (%)
T_1/2 (days)	27
AUC (ug/ml/hr)	45036
Clearance (L/h)	.009
Dosage (mg)	250
Metabolism	Unknown

↑ 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

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 ===Mechanism of Action===
-When [[HIV]] first infects someone, it directs the synthesis of several polyproteins. The maturation of the virus to its infectious form requires that these polyproteins be cleaved to their component proteins by [[HIV Protease]]. The subunits of <scene name='Amprenavir/Protease/1'>HIV Protease</scene> come together to form a catalytic tunnel capable of tightly binding the nascent peptides and cleaving them into their mature, infectious form. Within this tunnel lies <scene name='Amprenavir/Proteasec/1'>two Asp-Thr-Gly conserved sequences</scene>, which contain the <scene name='Amprenavir/Proteasecas/2'>catalytic Asp residues</scene>. These catalytic Asp residues carry out the hydrolytic cleavage of the polyprotein. Amprenavir <scene name='Amprenavir/Bound/1'>binds specifically</scene> to these conserved sequences within the HIV Protease tunnel, preventing the nascent polyproteins from entering. Unable to actively cleave the nascent proteins into their infectious form, HIV is unable to mature and proliferate, allowing the patients immune system to fight off the infection more easily.<ref>PMID:1799632</ref><ref>doi:10.1038/nrd1907</ref>
 ===Pharmacokinetics===