Idarucizumab

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Idarucizumab
Monoclonal antibody
TypeFab fragment
SourceHumanized (from mouse)
TargetDabigatran
Clinical data
Trade namesPraxbind
Other namesBI-655075
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: B2
Routes of
administration		Intravenous
ATC code
Legal status
Legal status
Identifiers
CAS Number
IUPHAR/BPS
DrugBank
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC2131H3299N555O671S11
Molar mass47782.71 g·mol−1

Idarucizumab, sold under the brand name Praxbind, is a monoclonal antibody used as a reversal agent for dabigatran.[4]

Idarucizumab was developed by Boehringer Ingelheim. One study sponsored by the manufacturer found that idarucizumab effectively reversed anticoagulation caused by dabigatran within minutes.[6]

It was approved for medical use in the United States and in the European Union in 2015.[7][4][5]

Mechanism of Action[edit]

Idarucizumab is a non-competitive inhibitor that forms complexes with dabigatran to counteract its anticoagulant effect within minutes of administration.[8] It binds to dabigatran that is free or bound to thrombin, as well as dabigatran's active metabolites.[9] Idarucizumab is specific to dabigatran and has an affinity that is around 350 times stronger compared to thrombin.[8]

Medical Uses[edit]

A systematic review found that idarucizumab was most frequently given to patients on dabigatran who were experiencing bleeding. It was also prescribed to patients before undergoing invasive surgery. The most common dose of idarucizumab prescribed was 5 g.[10] This is consistent with the current guidelines in the USA and Canada regarding the use and indications of idarucizumab.[11][12]

A second dose of idarucizumab may be administered if bleeding is still present, or if another invasive surgery is needed after the initial 5 g dose.[13] However, there is much less evidence on the benefits and harms of a repeated dose, and it is rarely given.[10][13]

Adverse Effects[edit]

The most common minor adverse effect was headache. Other side effects include back pain, skin irritation, constipation and weakness.[9]

A major adverse effect is thromboembolism resulting in stroke, pulmonary embolism, deep vein thrombosis and heart attack.[10] This is especially of concern, because patients prescribed idarucizumab were already at a higher risk of thromboembolic events.[13]

Pregnancy[edit]

There are no human or animal studies that show the effect of idarucizumab in pregnancy and lactation. Idarucizumab, if indicated, may be taken during pregnancy, due to the benefits it provides to the patient compared to the unclear risk to the fetus.[14]

Society and culture[edit]

Names[edit]

Idarucizumab is the International nonproprietary name (INN).[15] The description was updated in 2016.[16] Idarucizumab is the United States Adopted Name (USAN).[17]

References[edit]

  1. ^ "Prescription medicines: registration of new chemical entities in Australia, 2016". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
  2. ^ "Health Canada New Drug Authorizations: 2016 Highlights". Health Canada. 14 March 2017. Retrieved 7 April 2024.
  3. ^ "Praxbind 2.5 g/50 mL solution for injection/infusion - Summary of Product Characteristics (SmPC)". (emc). 1 July 2022. Retrieved 1 July 2022.
  4. ^ a b c "Praxbind- idarucizumab injection". DailyMed. 1 December 2019. Retrieved 19 August 2020.
  5. ^ a b "Praxbind EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 16 October 2020.
  6. ^ Pollack CV, Reilly PA, Eikelboom J, Glund S, Verhamme P, Bernstein RA, et al. (August 2015). "Idarucizumab for Dabigatran Reversal". The New England Journal of Medicine. 373 (6): 511–20. doi:10.1056/NEJMoa1502000. PMID 26095746.
  7. ^ "FDA approves Praxbind, the first reversal agent for the anticoagulant Pradaxa". U.S. Food and Drug Administration (FDA) (Press release). Archived from the original on 2015-10-17. Retrieved 2015-10-17.
  8. ^ a b Eikelboom, John W.; Quinlan, Daniel J.; van Ryn, Joanne; Weitz, Jeffrey I. (2015-12-22). "Idarucizumab: The Antidote for Reversal of Dabigatran". Circulation. 132 (25): 2412–2422. doi:10.1161/CIRCULATIONAHA.115.019628. ISSN 1524-4539. PMID 26700008.
  9. ^ a b Thibault, Nathan; Morrill, Amanda M.; Willett, Kristine C. (2018). "Idarucizumab for Reversing Dabigatran-Induced Anticoagulation: A Systematic Review". American Journal of Therapeutics. 25 (3): e333–e338. doi:10.1097/MJT.0000000000000460. ISSN 1536-3686. PMID 27175894.
  10. ^ a b c van der Horst, S. F. B.; Martens, E. S. L.; den Exter, P. L.; Bos, M. H. A.; van Mens, T. E.; Huisman, M. V.; Klok, F. A. (2023-05-29). "Idarucizumab for dabigatran reversal: A systematic review and meta-analysis of indications and outcomes". Thrombosis Research. 228: 21–32. doi:10.1016/j.thromres.2023.05.020. ISSN 1879-2472. PMID 37267671.
  11. ^ "Thrombosis Canada". thrombosiscanada.ca. Retrieved 2024-05-01.
  12. ^ Writing Committee Members; Joglar, José A.; Chung, Mina K.; Armbruster, Anastasia L.; Benjamin, Emelia J.; Chyou, Janice Y.; Cronin, Edmond M.; Deswal, Anita; Eckhardt, Lee L.; Goldberger, Zachary D.; Gopinathannair, Rakesh; Gorenek, Bulent; Hess, Paul L.; Hlatky, Mark; Hogan, Gail (2024-01-02). "2023 ACC/AHA/ACCP/HRS Guideline for the Diagnosis and Management of Atrial Fibrillation: A Report of the American College of Cardiology/American Heart Association Joint Committee on Clinical Practice Guidelines". Journal of the American College of Cardiology. 83 (1): 109–279. doi:10.1016/j.jacc.2023.08.017. ISSN 1558-3597. PMID 38043043.
  13. ^ a b c "DailyMed - PRAXBIND- idarucizumab injection". dailymed.nlm.nih.gov. Retrieved 2024-05-01.
  14. ^ Briggs, Gerald G.; Freeman, Roger K.; Towers, Craig V.; Forinash, Alicia B. (2017). Drugs in pregnancy and lactation: a reference guide to fetal and neonatal risk (11th ed.). Philadelphia, PA: Wolters Kluwer. ISBN 978-1-4963-4962-0. OCLC 951509534.
  15. ^ World Health Organization (2014). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 71". WHO Drug Information. 28 (1): 90–91. hdl:10665/331151.
  16. ^ World Health Organization (2016). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 76". WHO Drug Information. 30 (3): 544. hdl:10665/331020.
  17. ^ Statement On A Nonproprietary Name Adopted By The USAN Council - Idarucizumab Archived 2015-06-27 at the Wayback Machine, American Medical Association.
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