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
Db09264
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
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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
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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.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Idarucizumab which could result in a higher serum level.
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Idarucizumab.
AcarboseAcarbose may decrease the excretion rate of Idarucizumab which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Idarucizumab which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Idarucizumab which could result in a higher serum level.
AcetaminophenAcetaminophen may decrease the excretion rate of Idarucizumab which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Idarucizumab which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Idarucizumab which could result in a higher serum level.
AclidiniumAclidinium may decrease the excretion rate of Idarucizumab which could result in a higher serum level.
AcrivastineIdarucizumab may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Additional Data Available
  • Extended Description
    Extended Description
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    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity
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    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level
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    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action
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Food Interactions
Not Available

Products

Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
PraxbindInjection50 mg/1mLIntravenousBoehringer Ingelheim Pharmaceuticals, Inc.2015-10-21Not applicableUS flag
PraxbindInjection, solution2.5 g/50mLIntravenousBoehringer Ingelheim2016-09-08Not applicableEU flag
PraxbindSolution50 mgIntravenousBoehringer Ingelheim (Canada) Ltd Ltee2016-05-24Not applicableCanada flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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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

Chemical Identifiers

UNII
97RWB5S1U6
CAS number
1362509-93-0

References

General References
  1. 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]
  2. Yogaratnam D, Ditch K, Medeiros K, Doyno C, Fong JJ: Idarucizumab for Reversal of Dabigatran. Ann Pharmacother. 2016 Jul 7. pii: 1060028016659504. [PubMed:27389324]
KEGG Drug
D10741
PubChem Substance
347910427
RxNav
1716191
RxList
RxList Drug Page
Wikipedia
Idarucizumab
AHFS Codes
  • 20:28.92 — Antihemorrhagic Agents, Miscellaneous
FDA label
Download (227 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentHemorrhage4
1CompletedTreatmentHealthy Volunteers3
1CompletedTreatmentHemorrhage1
Not AvailableCompletedNot AvailableThromboembolism1
Not AvailableRecruitingNot AvailableIntracranial Hemorrhages1
Not AvailableWithdrawnNot AvailableHemorrhage1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionIntravenous50 mg/1mL
Injection, solutionIntravenous2.5 g/50mL
SolutionIntravenous50 mg
InjectionIntravenous50 mg/ml
Injection, solutionIntravenous50 mg/ml
Solution, concentrateIntravenous50 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