Idarucizumab Explained

Type:mab
Mab Type:Fab
Source:zu/o
Target:Dabigatran
Tradename:Praxbind
Dailymedid:Idarucizumab
Pregnancy Au:B2
Routes Of Administration:Intravenous
Atc Prefix:V03
Atc Suffix:AB37
Legal Au:S4
Legal Au Comment:[1]
Legal Ca:Rx-only
Legal Ca Comment:[2]
Legal Uk:POM
Legal Uk Comment:[3]
Legal Us:Rx-only
Legal Eu:Rx-only
Legal Eu Comment:[4]
Cas Number:1362509-93-0
Iuphar Ligand:8298
Drugbank:DB09264
Chemspiderid:none
Unii:97RWB5S1U6
Kegg:D10741
Synonyms:BI-655075
C:2131
H:3299
N:555
O:671
S:11

Idarucizumab, sold under the brand name Praxbind, is a monoclonal antibody used as a reversal agent for dabigatran.[5]

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]

Mechanism of action

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.

Medical uses

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.

Adverse effects

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

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

Pregnancy

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

Names

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

Notes and References

  1. Web site: Prescription medicines: registration of new chemical entities in Australia, 2016 . Therapeutic Goods Administration (TGA) . 21 June 2022 . 10 April 2023.
  2. Web site: Health Canada New Drug Authorizations: 2016 Highlights . . 14 March 2017 . 7 April 2024.
  3. Web site: Praxbind 2.5 g/50 mL solution for injection/infusion - Summary of Product Characteristics (SmPC) . (emc) . 1 July 2022 . 1 July 2022.
  4. Web site: Praxbind EPAR . European Medicines Agency (EMA) . 17 September 2018 . 16 October 2020.
  5. Web site: Praxbind- idarucizumab injection . DailyMed . U.S. National Library of Medicine . 1 December 2019 . 19 August 2020.
  6. Pollack CV, Reilly PA, Eikelboom J, Glund S, Verhamme P, Bernstein RA, Dubiel R, Huisman MV, Hylek EM, Kamphuisen PW, Kreuzer J, Levy JH, Sellke FW, Stangier J, Steiner T, Wang B, Kam CW, Weitz JI . Idarucizumab for Dabigatran Reversal . The New England Journal of Medicine . 373 . 6 . 511–520 . August 2015 . 26095746 . 10.1056/NEJMoa1502000 . free .
  7. FDA approves Praxbind, the first reversal agent for the anticoagulant Pradaxa. U.S. Food and Drug Administration (FDA). 2015-10-17. 2015-10-17. https://web.archive.org/web/20151017133421/https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm467300.htm. dead.
  8. Eikelboom JW, Quinlan DJ, van Ryn J, Weitz JI . Idarucizumab: The Antidote for Reversal of Dabigatran . Circulation . 132 . 25 . 2412–2422 . December 2015 . 26700008 . 10.1161/CIRCULATIONAHA.115.019628 .
  9. Thibault N, Morrill AM, Willett KC . Idarucizumab for Reversing Dabigatran-Induced Anticoagulation: A Systematic Review . American Journal of Therapeutics . 25 . 3 . e333–e338 . 2018 . 27175894 . 10.1097/MJT.0000000000000460 .
  10. van der Horst SF, Martens ES, den Exter PL, Bos MH, van Mens TE, Huisman MV, Klok FA . Idarucizumab for dabigatran reversal: A systematic review and meta-analysis of indications and outcomes . Thrombosis Research . 228 . 21–32 . August 2023 . 37267671 . 10.1016/j.thromres.2023.05.020 . free .
  11. Web site: Thrombosis Canada . 2024-05-01 . thrombosiscanada.ca.
  12. Joglar JA, Chung MK, Armbruster AL, Benjamin EJ, Chyou JY, Cronin EM, Deswal A, Eckhardt LL, Goldberger ZD, Gopinathannair R, Gorenek B, Hess PL, Hlatky M, Hogan G, Ibeh C, Indik JH, Kido K, Kusumoto F, Link MS, Linta KT, Marcus GM, McCarthy PM, Patel N, Patton KK, Perez MV, Piccini JP, Russo AM, Sanders P, Streur MM, Thomas KL, Times S, Tisdale JE, Valente AM, Van Wagoner DR . 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 . January 2024 . 38043043 . 10.1016/j.jacc.2023.08.017 . 11104284 .
  13. Web site: DailyMed - PRAXBIND- idarucizumab injection . 2024-05-01 . dailymed.nlm.nih.gov.
  14. Book: Briggs GG, Freeman RK, Towers CV, Forinash AB . Drugs in pregnancy and lactation: a reference guide to fetal and neonatal risk . 2017 . Wolters Kluwer . 978-1-4963-4962-0 . 11th . Philadelphia, PA . 951509534.
  15. ((World Health Organization)) . 2014 . International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 71 . WHO Drug Information . 28 . 1 . 90–91 . 10665/331151 . free . World Health Organization .
  16. ((World Health Organization)) . 2016 . International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 76 . WHO Drug Information . 30 . 3 . 544 . 10665/331020 . free . World Health Organization .
  17. Web site: Idarucizumab . Statement On A Nonproprietary Name Adopted By The USAN Council . https://web.archive.org/web/20150627024121/http://www.ama-assn.org/resources/doc/usan/x-pub/idarucizumab.pdf . 2015-06-27 . .

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