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

• Anticoagulant effects of dabigatran

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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
Unlock Additional Data
Abacavir	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 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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Action
Action
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An effect category for each drug interaction. Know how this interaction affects the subject drug.
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Food Interactions

Not Available

Products

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Unlock Additional Data
Praxbind	Injection	50 mg/1mL	Intravenous	Boehringer Ingelheim Pharmaceuticals, Inc.	2015-10-21	Not applicable
Praxbind	Injection, solution	2.5 g/50mL	Intravenous	Boehringer Ingelheim	2016-09-08	Not applicable
Praxbind	Solution	50 mg	Intravenous	Boehringer Ingelheim (Canada) Ltd Ltee	2016-05-24	Not applicable

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

• V03AB — Antidotes
• V03A — ALL OTHER THERAPEUTIC PRODUCTS
• V03 — ALL OTHER THERAPEUTIC PRODUCTS
• V — VARIOUS

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

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]

External Links

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

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

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Drug created on October 27, 2015 12:45 / Updated on January 25, 2021 22:38