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9.7 MiB
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9.7 MiB
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[{"ID":"DB00001","Name":"Lepirudin","DrugType":"biotech","HalfLife":"Approximately 1.3 hours","Description":"Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells. Bayer ceased the production of lepirudin (Refludan) effective May 31, 2012.","Classification":{"Description":"","DirectParent":"Peptides","Kingdom":"Organic Compounds","SuperClass":"Organic Acids","Class":"Carboxylic Acids and Derivatives","SubClass":"Amino Acids, Peptides, and Analogues"},"Indication":"For the treatment of heparin-induced thrombocytopenia","Toxicity":"In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.","MechanismOfAction":"Lepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade. ","Pharmacodynamics":"Lepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches.","Absorption":"Bioavailability is 100% following injection.","Interactions":[{"ID":"DB01381"},{"ID":"DB00374"}],"Salts":null,"Groups":{"approved":true},"Pathways":[{"ID":"SMP00278","Drugs":["DB00001","DB01373"]}]},{"ID":"DB00002","Name":"Cetuximab","DrugType":"biotech","HalfLife":"114 hrs","Description":"Epidermal growth factor receptor binding FAB. Cetuximab is composed of the Fv (variable; antigen-binding) regions of the 225 murine EGFr monoclonal antibody specific for the N-terminal portion of human EGFr with human IgG1 heavy and kappa light chain constant (framework) regions.","Classification":{"Description":"","DirectParent":"Peptides","Kingdom":"Organic Compounds","SuperClass":"Organic Acids","Class":"Carboxylic Acids and Derivatives","SubClass":"Amino Acids, Peptides, and Analogues"},"Indication":"For treatment of EGFR-expressing metastatic colorectal cancer in patients who are refractory to other irinotecan-based chemotherapy regimens. Cetuximab is also indicated for treatment of squamous cell carcinoma of the head and neck in conjucntion with radiation therapy.","Toxicity":"Single doses of cetuximab higher than 500 mg/m\u003csup\u003e2\u003c/sup\u003e have not been tested. There is no experience with overdosage in human clinical trials.\r\n\r\n","MechanismOfAction":"Cetuximab binds to the epidermal growth factor receptor (EGFr) on both normal and tumor cells. EGFr is over-expressed in many colorectal cancers. Cetuximab competitively inhibits the binding of epidermal growth factor (EGF) and TGF alpha, thereby reducing their effects on cell growth and metastatic spread.","Pharmacodynamics":"Used in the treatment of colorectal cancer, cetuximab binds specifically to the epidermal growth factor receptor (EGFr, HER1, c-ErbB-1) on both normal and tumor cells. EGFr is over-expressed in many colorectal cancers. Cetuximab competitively inhibits the binding of epidermal growth factor (EGF) and other ligands, such as transforming growth factor–alpha. Binding of cetuximab to the EGFr blocks phosphorylation and activation of receptor-associated kinases, resulting in inhibition of cell growth, induction of apoptosis, decreased matrix metalloproteinase secretion and reduced vascular endothelial growth factor production.","Absorption":"","Interactions":null,"Salts":null,"Groups":{"approved":true},"Pathways":[{"ID":"SMP00474","Drugs":["DB00002"]}]},{"ID":"DB00003","Name":"Dornase alfa","DrugType":"biotech","HalfLife":"","Description":"Dornase alfa is a biosynthetic form of human deoxyribunuclease I (DNase I) enzyme. It is produced in genetically modified Chinese hamster ovary (CH
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