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Synonyms: aDabi-Fab | BI 655075 | Praxbind®
idarucizumab is an approved drug (FDA and EMA (2015))
Compound class:
Antibody
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 |
| No information available. |
Summary of Clinical Use  |
| Following from FDA Breakthrough Therapy Designation, the FDA granted accelerated approval (October 2015) for idarucizumab to be used to reverse the anticoagulant effects of dabigatran in patients requiring emergency surgery or urgent procedures, or those suffering from life-threatening or uncontrolled bleeding. EMA approval for the same indications followed in November 2015. |
| Mechanism Of Action and Pharmacodynamic Effects |
| Results from a Phase I clinical trial (NCT01955720) indicate that idarucizumab rapidly and completely reverses the anticoagulant effect of dabigatran in healthy volunteers, with only mild adverse reactions (eg headache, erythema and migraine) reported [2]. |
| External links |
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For extended ADME data see the following: Electronic Medicines Compendium (eMC) Drugs.com European Medicines Agency (EMA) |
