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Primary information
ThPP ID	Th1061
Therapeutic Peptide/Protein Name	Trastuzumab
Sequence	Light chain 1: DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAW view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	145531.5
Chemical Formula	C6470H10012N1726O2013S42
Isoelectric Point	8.45
Hydrophobicity	-0.415
Melting Point (℃)	61 (FAB f
Half Life	average 28.5 days
Description	A recombinant IgG1 kappa, humanized monoclonal antibody that selectively binds with high affinity in a cell-based assay (Kd = 5 nM) to the extracellular domain of the human epidermal growth factor receptor protein. Produced in CHO cell culture.
Indication/Disease	For treatment of early stage HER2-positive breast cancer, or metastatic breast cancer that substantially overexpress HER2.
Pharmacodynamics	Used in the treatment of HER2-positive breast cancer. HER2 protein overexpression is observed in 25%-30% of primary breast cancers.Trastuzumab has been shown, in both in vitro assays and in animals, to inhibit the proliferation of human tumorcells that overexpress HER2. It is a mediator of antibody dependent cellular cytotoxicity, in that the binding of the antibody to HER2 overexpressing cells leads to preferential cell death.
Mechanism of Action	Trastuzumab binds to the HER2 (or c-erbB2) proto-oncogene, an EGF receptor-like protein found on 20-30% of breast cancer cells. The binding leads to antibody mediated (complement mediated) killing of the HER2 positive cells.
Toxicity	Administration of trastuzumab can result in ventricular dysfunction and congestive heart failure. Risk of cardiotocity is especially elevated in patients recieving concurrent anthracycline or cyclophosphamide therapy.
Metabolism	Most likely removed by opsonization via the reticuloendothelial system.
Absorption	N.A.
Volume of Distribution	44 mL/kg
Clearance	N.A.
Categories	Antineoplastic Agents
Patents Number	CA2103059
Date of Issue	23/03/09
Date of Expiry	16/06/16
Drug Interaction	Abciximab may increase the risk of a hypersensitivy reaction to Trastuzumab
Target	N.A.
Information of corresponding available drug in the market
Brand Name	Herceptin
Company	Genentech
Brand Discription	Herceptin (trastuzumab) is a humanized IgG1 kappa monoclonal antibody that selectively binds with high affinity to the extracellular domain of the human epidermal growth factor receptorÂ 2 protein, HER2. Trastuzumab is produced by recombinant DNA technology in a mammalian cell (Chinese Hamster Ovary) culture containing the antibiotic gentamicin
Prescribed for	Adjuvant Breast Cancer, Metastatic Breast Cancer, Metastatic Gastric Cancer
Chemical Name	N.A.
Formulation	Each multi-use vial of Herceptin contains 440 mg trastuzumab, 400 mg a,a-trehalose dihydrate, 9.9 mg L-histidine HCl, 6.4 mg L-histidine, and 1.8 mg polysorbate 20, USP. Reconstitution with 20 mL of the appropriate diluent (BWFI or SWFI) yields a solution containing 21 mg/mL trastuzumab, at a pH of approximately 6
Physcial Appearnce	Herceptin is a sterile, white to pale yellow, preservative-free lyophilized powder
Route of Administration	Â Intravenous administration
Recommended Dosage	Initial dose of 4mg/kg for 90 minutes and after that 2mg/kg weekly for 30 minutes during chemotherapy for the first 12 weeks incase of breast cancer. Last Dose 6mg/kg for 3 weeks.
Contraindication	None
Side Effects	Cardiomyopathy, Infusion reactions, Embryo-fetal Toxicity, Pulmonary toxicity,Exacerbation of chemotherapy-induced neutropenia, ever, nausea, vomiting, infusion reactions, diarrhea, infections, increased cough, headache, fatigue, dyspnea, rash, neutropenia, anemia, and myalgia.
Useful Link	http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=492dbdb2-077e-4064-bff3-372d6af0a7a2 http://www.rxlist.com/herceptin-drug.htm
PubMed ID	21813259, 14613027, 14528282, 12908564, 25572781, 25547504, 25532690, 25494663
3-D Structure	Th1061 (View) or (Download)