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1385 details
Primary information
ThPP IDTh1061
Therapeutic Peptide/Protein NameTrastuzumab
SequenceLight chain 1: DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAW view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight145531.5
Chemical FormulaC6470H10012N1726O2013S42
Isoelectric Point8.45
Hydrophobicity-0.415
Melting Point (℃)61 (FAB f
Half Lifeaverage 28.5 days
DescriptionA 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/DiseaseFor treatment of early stage HER2-positive breast cancer, or metastatic breast cancer that substantially overexpress HER2.
PharmacodynamicsUsed 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 ActionTrastuzumab 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.
ToxicityAdministration 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.
MetabolismMost likely removed by opsonization via the reticuloendothelial system.
AbsorptionN.A.
Volume of Distribution44 mL/kg
ClearanceN.A.
CategoriesAntineoplastic Agents
Patents NumberCA2103059
Date of Issue23/03/09
Date of Expiry16/06/16
Drug InteractionAbciximab may increase the risk of a hypersensitivy reaction to Trastuzumab
TargetN.A.
Information of corresponding available drug in the market
Brand NameHerceptin
CompanyGenentech
Brand DiscriptionHerceptin (trastuzumab) is a humanized IgG1 kappa monoclonal antibody that selectively binds with high affinity to the extracellular domain of the human epidermal growth factor receptor 2 protein, HER2. Trastuzumab is produced by recombinant DNA technology in a mammalian cell (Chinese Hamster Ovary) culture containing the antibiotic gentamicin
Prescribed forAdjuvant Breast Cancer, Metastatic Breast Cancer, Metastatic Gastric Cancer
Chemical NameN.A.
FormulationEach 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 AppearnceHerceptin is a sterile, white to pale yellow, preservative-free lyophilized powder
Route of Administration Intravenous administration
Recommended DosageInitial 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.
ContraindicationNone
Side EffectsCardiomyopathy, 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 Linkhttp://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=492dbdb2-077e-4064-bff3-372d6af0a7a2 http://www.rxlist.com/herceptin-drug.htm
PubMed ID21813259, 14613027, 14528282, 12908564, 25572781, 25547504, 25532690, 25494663
3-D StructureTh1061 (View) or (Download)