Desirudin
Identification
- Generic Name
- Desirudin
- DrugBank Accession Number
- DB11095
- Background
Desirudin is a direct inhibitor of human thrombin. It has a protein structure that is similar to that of hirudin, the naturally occurring anticoagulant present in the peripharyngeal glands in the medicinal leech, Hirudo medicinalis. Hirudin is a single polypeptide chain of 65 amino acids residues and contains three disulfide bridges. Desirudin has a chemical formula of C287H440N80O110S6 with a molecular weight of 6963.52.
It is mainly indicated for the prevention of deep vein thrombosis in hip replacement surgery patients. Common side effects include: Bleeding gums, collection of blood under the skin, coughing up blood, deep, dark purple bruise and difficulty with breathing or swallowing.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Other protein based therapies - Protein Chemical Formula
- C287H440N80O110S6
- Protein Average Weight
- Not Available
- Sequences
- Not Available
- Synonyms
- 63-Desulfohirudin
- 63-Desulfohirudin (Hirudo Medicinalis Isoform HV1)
- 63-Desulfohirudin (recombinant)
- Desirudin
- Desirudin recombinant
- Desirudina
- Hirudin desirudin
- External IDs
- CGP-39393
Pharmacology
- Indication
Indicated as prophylaxis of deep vein thrombosis for patients undergoing hip replacement surgery.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Prophylaxis of Deep vein thrombosis •••••••••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Desirudin results in dose-dependent prolongation of the activated partial thromboplastin time (aPTT).
- Mechanism of action
Desirudin is a direct, highly selective thrombin inhibitor. Reversibly binds to the active thrombin site of free and clot-associated thrombin. Inhibits fibrin formation, activation of coagulation factors V, VII, and XIII, and thrombin-induced platelet aggregation resulting in a dose-dependent prolongation of the activated partial thromboplastin time (aPTT).
- Absorption
Absorption is complete after subcutaneous administration. Time to peak in plasma is 1 to 3 hours.
- Volume of distribution
0.25 L/kg.
- Protein binding
Desirudin binds specifically and directly to thrombin, forming an extremely tight, non-covalent complex with an inhibitionconstant of approximately 2.6 x 10-13 M. Thus, free or protein bound desirudin immediately binds circulating thrombin.
- Metabolism
Human and animal data suggest that desirudin is primarily eliminated and metabolized by the kidney. The total urinary excretion of unchanged desirudin amounts to 40 to 50% of the administered dose. Metabolites lacking one or two C-terminal amino acids constitute a minor proportion of the material recovered from urine (< 7%). There is no evidence for the presence of other metabolites. This indicates that desirudin is metabolized by stepwise degradation from the C-terminus probably catalyzed by carboxypeptidase(s) such as carboxypeptidase A.
- Route of elimination
Urine (40% to 50% as unchanged drug).
- Half-life
~2 hours.
- Clearance
1.5 to 2.7 mL/min/kg.
- Adverse Effects
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- Toxicity
No data available.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of bleeding can be increased when Abciximab is combined with Desirudin. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Desirudin. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Desirudin is combined with Acemetacin. Acenocoumarol The risk or severity of bleeding can be increased when Acenocoumarol is combined with Desirudin. Acetylsalicylic acid Acetylsalicylic acid may increase the anticoagulant activities of Desirudin. - Food Interactions
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Iprivask Kit 30 mg/1mL Subcutaneous CANYON PHARMACEUTICALS, INC 2010-08-30 2014-05-09 US Iprivask Kit 30 mg/1mL Subcutaneous Valeant Pharmaceuticals North America LLC 2013-12-31 2018-07-31 US Iprivask Injection, powder, lyophilized, for solution 15 mg/100mg Subcutaneous Canyon Pharmaceuticals, Inc. 2010-06-10 2010-11-01 US Iprivask Kit 30 mg/1mL Subcutaneous Marathon Pharmaceuticals 2013-12-31 2016-08-31 US
Categories
- ATC Codes
- B01AE01 — Desirudin
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- U0JZ726775
- CAS number
- 120993-53-5
References
- General References
- External Links
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Thrombosis 1 4 Terminated Prevention Suspected Heparin-Induced Thrombocytopenia 1 2, 3 Completed Prevention Deep Vein Thrombosis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, lyophilized, for solution Subcutaneous 15 mg/100mg Kit Subcutaneous 30 mg/1mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Not Available
- Experimental Properties
- Not Available
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Zinc ion binding
- Specific Function
- Carboxypeptidase that catalyzes the release of a C-terminal amino acid, but has little or no action with -Asp, -Glu, -Arg, -Lys or -Pro.
- Gene Name
- CPA1
- Uniprot ID
- P15085
- Uniprot Name
- Carboxypeptidase A1
- Molecular Weight
- 47139.86 Da
Drug created at December 03, 2015 16:51 / Updated at February 21, 2021 18:52