idarucizumab

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Ligands
idarucizumab

GtoPdb Ligand ID: 8298

Synonyms: aDabi-Fab | BI 655075 | Praxbind®

idarucizumab is an approved drug (FDA and EMA (2015))

Comment: Idarucizumab is a fully humanized antigen-binding fragment (Fab) of an antibody binding to the active metabolite (dabigatran) of the anti-coagulant prodrug dabigatran etexilate [4]. Idarucizumab has been granted FDA Breakthrough Therapy Designation to help expedite its development, as it represents a solution to an unmet clinical need. That is, to be able to reverse the effects of newer direct, oral anticoagulants such as dabigatran etexilate on demand. Antidotes to other direct anticoagulants in development are discussed in [3] and [1] (see also andexanet alfa).
The crystal structure of dabigatran-bound idarucizumab has been resolved at 1.7Å (Protein Data Bank ID 4JN2) [5]. Additional information regarding the invention of idarucizumab is available in patent US8486398 [6].

View more information in the IUPHAR Pharmacology Education Project: idarucizumab

References
1. Costin J, Ansell J, Laulicht B, Bakhru S, Steiner S. (2014) Reversal agents in development for the new oral anticoagulants. Postgrad Med, 126 (7): 19-24. [PMID:25387210]
2. Glund S, Moschetti V, Norris S, Stangier J, Schmohl M, van Ryn J, Lang B, Ramael S, Reilly P. (2015) A randomised study in healthy volunteers to investigate the safety, tolerability and pharmacokinetics of idarucizumab, a specific antidote to dabigatran. Thromb Haemost, 113 (5): 943-51. [PMID:25789661]
3. Gomez-Outes A, Suarez-Gea ML, Lecumberri R, Terleira-Fernandez AI, Vargas-Castrillon E. (2014) Specific antidotes in development for reversal of novel anticoagulants: a review. Recent Pat Cardiovasc Drug Discov, 9 (1): 2-10. [PMID:25494843]
4. Schiele F, van Ryn J, Canada K, Newsome C, Sepulveda E, Park J, Nar H, Litzenburger T. (2013) A specific antidote for dabigatran: functional and structural characterization. Blood, 121 (18): 3554-62. [PMID:23476049]
5. Schiele F, van Ryn J, Litzenburger T, Ritter M, Seeliger D, Nar H. (2015) Structure-guided residence time optimization of a dabigatran reversal agent. MAbs, 7 (5): 871-80. [PMID:26047352]
6. Van Ryn J, Park JE, Hauel N, Kunz U, Litzenburger T, Canada K, Singh S, Waterman A. (2013) Anticoagulant antidotes comprising antibodies that bind dabigatran and/or related compounds. Patent number: US8486398. Assignee: Boehringer Ingelheim International Gmbh. Priority date: 20/01/2010. Publication date: 16/07/2013.

References

1. Costin J, Ansell J, Laulicht B, Bakhru S, Steiner S. (2014)
Reversal agents in development for the new oral anticoagulants.
Postgrad Med, 126 (7): 19-24. [PMID:25387210]

2. Glund S, Moschetti V, Norris S, Stangier J, Schmohl M, van Ryn J, Lang B, Ramael S, Reilly P. (2015)
A randomised study in healthy volunteers to investigate the safety, tolerability and pharmacokinetics of idarucizumab, a specific antidote to dabigatran.
Thromb Haemost, 113 (5): 943-51. [PMID:25789661]

3. Gomez-Outes A, Suarez-Gea ML, Lecumberri R, Terleira-Fernandez AI, Vargas-Castrillon E. (2014)
Specific antidotes in development for reversal of novel anticoagulants: a review.
Recent Pat Cardiovasc Drug Discov, 9 (1): 2-10. [PMID:25494843]

4. Schiele F, van Ryn J, Canada K, Newsome C, Sepulveda E, Park J, Nar H, Litzenburger T. (2013)
A specific antidote for dabigatran: functional and structural characterization.
Blood, 121 (18): 3554-62. [PMID:23476049]

5. Schiele F, van Ryn J, Litzenburger T, Ritter M, Seeliger D, Nar H. (2015)
Structure-guided residence time optimization of a dabigatran reversal agent.
MAbs, 7 (5): 871-80. [PMID:26047352]

6. Van Ryn J, Park JE, Hauel N, Kunz U, Litzenburger T, Canada K, Singh S, Waterman A. (2013)
Anticoagulant antidotes comprising antibodies that bind dabigatran and/or related compounds.
Patent number: US8486398. Assignee: Boehringer Ingelheim International Gmbh. Priority date: 20/01/2010. Publication date: 16/07/2013.