Idarucizumab
Identification
- Summary
Idarucizumab is an antibody that binds dabigatran for the reversal of anticoagulant effects of dabigatran.
- Brand Names
- Praxbind
- Generic Name
- Idarucizumab
- DrugBank Accession Number
- DB09264
- Background
Idarucizumab is a humanized monoclonal antibody fragment (Fab) derived from an immunoglobulin G1 isotype molecule that binds to and inactivates the oral anticoagulant dabigatran, thereby reversing its anticoagulant effect. As a direct acting oral anticoagulant (DOAC), one of the risks associated with the use of dabigatran includes bleeding, espeically when given to patients at increased risk (elderly, chronic kidney disease, concomitant NSAID or warfarin use, etc).
Approved under the tradename Praxbind (FDA), idarucizumab is indicated for the emergency treatment of dabigatran-associated bleeding in life-threatening or surgically induced situations. Its use is associated with immediate, complete and sustained reversal of the anticoagulant effects of dabigatran.
Idarucizumab protein structure can be viewed below, with disulfide bridges at the following points: H22-H95, H149-H205, H225-L-219, L23-L93, L139-L199.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Structure
- Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
>Heavy Chain QVQLQESGPGLVKPSETLSLTCTVSGFSLTSYIVDWIRQPPGKGLEWIGVIWAGGSTGYN SALRSRVSITKDTSKNQFSLKLSSVTAADTAVYYCASAAYYSYYNYDGFAYWGQGTLVTV SSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQ SSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSC
>Light Chain DVVMTQSPLSLPVTLGQPASISCKSSQSLLYTDGKTYLYWFLQRPGQSPRRLIYLVSKLD SGVPDRFSGSGSGTDFTLKISRVEAEDVGVYYCLQSTHFPHTFGGGTKVEIKRTVAAPSV FIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSL SSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format- Synonyms
- aDabi-Fab
- Idarucizumab
- External IDs
- BI 655075
- BI-655075
- BI655075
Pharmacology
- Indication
For use in patients treated with Dabigatran when reversal of the anticoagulant effects of dabigatran is needed for emergency surgery/urgent procedures and in life-threatening or uncontrolled bleeding.
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- Contraindications & Blackbox Warnings
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- Pharmacodynamics
Not Available
- Mechanism of action
Idarucizumab is a specific reversal agent for dabigatran. It is a humanized monoclonal antibody fragment (Fab) that binds to dabigatran and its acylglucuronide metabolites with higher affinity than the binding affinity of dabigatran to thrombin, neutralizing their anticoagulant effect.
- Absorption
Not Available
- Volume of distribution
8.9 L
- Protein binding
Not Available
- Metabolism
Several pathways have been described that may contribute to the metabolism of antibodies. All of these pathways involve biodegradation of the antibody to smaller molecules, i.e., small peptides or amino acids which are then reabsorbed and incorporated in the general protein synthesis.
- Route of elimination
After intravenous administration of 5 g idarucizumab, 32.1% (gCV 60.0%) of the dose was recovered in urine within a collection period of 6 hours and less than 1% in the following 18 hours. The remaining part of the dose is assumed to be eliminated via protein catabolism, mainly in the kidney.
- Half-life
initial half-life: 47 minutes terminal half-life: 10.3 h
- Clearance
47.0 mL/min
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
In healthy volunteers, the most frequently reported adverse reactions in greater than or equal to 5% of subjects treated with idarucizumab was headache. In patients, the most frequently reported adverse reactions in greater than or equal to 5% of patients treated with idarucizumab were hypokalemia, delirium, constipation, pyrexia, and pneumonia.
- 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 softwareAbacavir Abacavir may decrease the excretion rate of Idarucizumab which could result in a higher serum level. Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Idarucizumab. Aceclofenac Aceclofenac may decrease the excretion rate of Idarucizumab which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Idarucizumab which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Idarucizumab which could result in a higher serum level. Acetazolamide Acetazolamide may increase the excretion rate of Idarucizumab which could result in a lower serum level and potentially a reduction in efficacy. Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Idarucizumab which could result in a higher serum level. Aclidinium Aclidinium may decrease the excretion rate of Idarucizumab which could result in a higher serum level. Acrivastine Idarucizumab may decrease the excretion rate of Acrivastine which could result in a higher serum level. Acyclovir Acyclovir may decrease the excretion rate of Idarucizumab which could result in a higher serum level. Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- No interactions found.
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 Praxbind Injection, solution 2.5 g/50mL Intravenous Boehringer Ingelheim 2016-09-08 Not applicable EU Praxbind Solution 50 mg / mL Intravenous Boehringer Ingelheim (Canada) Ltd Ltee 2016-05-24 Not applicable Canada Praxbind Injection 50 mg/1mL Intravenous Boehringer Ingelheim Pharmaceuticals, Inc. 2015-10-21 Not applicable US
Categories
- ATC Codes
- V03AB37 — Idarucizumab
- 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
- Humans and other mammals
Chemical Identifiers
- UNII
- 97RWB5S1U6
- CAS number
- 1362509-93-0
References
- General References
- Syed YY: Idarucizumab: A Review as a Reversal Agent for Dabigatran. Am J Cardiovasc Drugs. 2016 Aug;16(4):297-304. doi: 10.1007/s40256-016-0181-4. [Article]
- Yogaratnam D, Ditch K, Medeiros K, Doyno C, Fong JJ: Idarucizumab for Reversal of Dabigatran. Ann Pharmacother. 2016 Jul 7. pii: 1060028016659504. [Article]
- External Links
- KEGG Drug
- D10741
- PubChem Substance
- 347910427
- 1716191
- RxList
- RxList Drug Page
- Wikipedia
- Idarucizumab
- FDA label
- Download (227 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Completed Treatment Hemorrhage 4 1 Completed Treatment Healthy Subjects (HS) 3 1 Completed Treatment Hemorrhage 1 Not Available Completed Not Available Hemorrhage 1 Not Available Completed Not Available Intracranial Hemorrhages 1 Not Available Completed Not Available Thromboembolism 1 Not Available Withdrawn Not Available Hemorrhage 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intravenous Injection Intravenous 50 mg/1mL Solution Intravenous 50 mg / mL Injection Intravenous 50 mg/ml Injection, solution Intravenous Injection, solution Intravenous 50.00 mg/ml Solution, concentrate Intravenous 50 mg Injection, solution Intravenous 2.5 g/50ml - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Drug created at October 27, 2015 18:45 / Updated at June 03, 2022 07:24