| Generic name |
Lepirudin
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| Brand Names/Synonyms |
Hirudin variant-1;Lepirudin; Refludan (Berlex Labs) |
| Indication |
For treatment of heparin-induced thrombocytopenia |
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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. |
| Pharmacology |
Used to break up clots and to reduce thrombocytopenia. Hirudin binds to thrombin and prevents thrombus or clot formation. Hirudin is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Hirudin requires no cofactor for its anticoagulant action. |
| Mechanism Of Action |
Hirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. |
Lepirudin News
(When available) |
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| Dosage Forms |
POWDER FOR SOLUTION |
| Drug_Category |
Anticoagulants; Antithrombotic Agents; unclassified therapeutic agents (92:00.00) |
| Absorption |
Not Available |
| Interactions |
Not Available |
| Toxicity |
Not Available |
| Organisms Affected |
Humans and other mammals |
| Chemical IUPAC Name |
Hirudo medicinalis hirudin (variant 1) |
| Chemical Formula |
C288H448N80O110S6 |
| Molecular Weight |
6983.5 |
| Smiles String |
Not Available |
| Melting Point |
65 oC (Otto, A. & Seckler, R. Eur. J. Biochem. 202:67-73 (1991)) |
| Water Solubility |
Not Available |
| State |
Transparent, slightly viscous, aqueous liquid |
| LogP/Hphobicity |
-0.777 |
| Isoelectric Point |
4.04 |
| Biotransformation |
Not Available |
| Half Life |
~1.3 hours |
| Protein Binding [%] |
Not Available |
| RxList Link |
RXlist |
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| Drug Reference |
http://www.rxlist.com/cgi/generic3/lepirudin.htm |
| Drug Type |
Approved Drug |
| Accession No |
BIOD00024 |
| CAS Registry Number |
120993-53-5 |
| KEGG Compound ID |
Not Available |
| PubChem ID |
Not Available |
| PharmGKB ID |
PA450195 |
| SwissProt ID |
ITH1_HIRME (P01050) |
| GenBank ID |
Not Available |
| Drug ID Number [DIN] |
2240996
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