Idarucizumab
Identification
- Name
- Idarucizumab
- Accession Number
- DB09264
- Description
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
- 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.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- 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
Learn about our commercial Adverse Effects data.
Learn More- 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.
- Affected organisms
- Humans and other mammals
- 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 Unlock Additional DataAbacavir 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. Acarbose Acarbose may decrease the excretion rate of Idarucizumab which could result in a higher serum level. 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. Additional Data Available- Extended DescriptionExtended DescriptionAvailable for Purchase
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - SeveritySeverityAvailable for Purchase
A severity rating for each drug interaction, from minor to major.
Learn more - Evidence LevelEvidence LevelAvailable for Purchase
A rating for the strength of the evidence supporting each drug interaction.
Learn more - ActionActionAvailable for Purchase
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Not Available
Products
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataPraxbind Injection 50 mg/1mL Intravenous Boehringer Ingelheim Pharmaceuticals, Inc. 2015-10-21 Not applicable US Praxbind Injection, solution 2.5 g/50mL Intravenous Boehringer Ingelheim 2016-09-08 Not applicable EU Praxbind Solution 50 mg Intravenous Boehringer Ingelheim (Canada) Ltd Ltee 2016-05-24 Not applicable Canada Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
Categories
- ATC Codes
- V03AB37 — Idarucizumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antidotes
- Antihemorrhagic Agents, Miscellaneous
- Blood Proteins
- Drugs that are Mainly Renally Excreted
- Globulins
- Humanized Monoclonal Antibody Fragment
- Immunoglobulins
- Immunoproteins
- Proteins
- Serum Globulins
- 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
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. [PubMed:27388764]
- Yogaratnam D, Ditch K, Medeiros K, Doyno C, Fong JJ: Idarucizumab for Reversal of Dabigatran. Ann Pharmacother. 2016 Jul 7. pii: 1060028016659504. [PubMed:27389324]
- External Links
- KEGG Drug
- D10741
- PubChem Substance
- 347910427
- 1716191
- RxList
- RxList Drug Page
- Wikipedia
- Idarucizumab
- AHFS Codes
- 20:28.92 — Antihemorrhagic Agents, Miscellaneous
- FDA label
- Download (227 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 3 Completed Treatment Hemorrhage 4 1 Completed Treatment Healthy Volunteers 3 1 Completed Treatment Hemorrhage 1 Not Available Completed Not Available Thromboembolism 1 Not Available Recruiting Not Available Intracranial Hemorrhages 1 Not Available Withdrawn Not Available Hemorrhage 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intravenous 50 mg/1mL Injection, solution Intravenous 2.5 g/50mL Solution Intravenous 50 mg Injection Intravenous 50 mg/ml Injection, solution Intravenous 50 mg/ml Solution, concentrate Intravenous 50 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Drug created on October 27, 2015 12:45 / Updated on January 25, 2021 22:38