Idarucizumab

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.

• PRAXBIND is indicated in patients treated with Pradaxa when reversal of the anticoagulant effects of dabigatran is needed: For emergency surgery/urgent procedures In life-threatening or uncontrolled bleeding PRAXBIND is a humanized monoclonal antibody fragment (Fab) indicated in patients treated with Pradaxa ® when reversal of the anticoagulant effects of dabigatran is needed: For emergency surgery/urgent procedures In life-threatening or uncontrolled bleeding ( 1 )

• None.contraindicated

For intravenous use only. The recommended dose of PRAXBIND is 5 g, provided as two separate vials each containing 2.5 g/50 mL idarucizumab. ( 2.1 ) There is limited data to support administration of an additional 5 g of PRAXBIND. ( 2.1 ) 2.1 Recommended Dose The recommended dose of PRAXBIND is 5 g, provided as two separate vials each containing 2.5 g/50 mL idarucizumab (see Figure 1 ). Both vials are packaged together in one carton. For intravenous use only. There is limited data to support administration of an additional 5 g of PRAXBIND [see Warnings and Precautions (5.2) ]. 2.2 Preparation Remove both vials (each containing 2.5 g/50 mL idarucizumab) from carton. Ensure aseptic handling when preparing the infusion. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Once solution has been removed from the vial, administration should begin promptly. The solution in vials may be stored at room temperature, 25°C (77°F), but must be used within 6 hours [see How Supplied/Storage and Handling (16.2) ] . 2.3 Administration Do not mix with other medicinal products. Use aseptic technique when administering PRAXBIND. Intravenously administer the dose of 5 g (2 vials, each contains 2.5 g) as Two consecutive infusions (see Figure 2 ) or Bolus injection by injecting both vials consecutively one after another via syringe (see Figure 3 ). A pre-existing intravenous line may be used for administration of PRAXBIND.

Thromboembolic Risk: Reversing dabigatran therapy exposes patients to the thrombotic risk of their underlying disease. Resume anticoagulant therapy as soon as medically appropriate. ( 2.4 , 5.1 ) Re-elevation of Coagulation Parameters: In patients with elevated coagulation parameters and reappearance of clinically relevant bleeding or requiring a second emergency surgery/urgent procedure, an additional 5 g dose of PRAXBIND may be considered. ( 5.2 ) Hypersensitivity reactions: Discontinue administration and evaluate. ( 5.3 ) Risks of Serious Adverse Reactions in Patients with Hereditary Fructose Intolerance due to Sorbitol Excipient: Patients with hereditary fructose intolerance may be at risk of adverse reactions. ( 5.4 ) 5.1 Thromboembolic Risk Patients being treated with dabigatran therapy have underlying disease states that predispose them to thromboembolic events. Reversing dabigatran therapy exposes patients to the thrombotic risk of their underlying disease. To reduce this risk, resumption of anticoagulant therapy should be considered as soon as medically appropriate [see Dosage and Administration (2.4) ]. 5.2 Re-elevation of Coagulation Parameters In a limited number of patients in the clinical program, between 12 and 24 hours after administration of 5 g idarucizumab, elevated coagulation parameters (e.g., activated partial thromboplastin time (aPTT) or ecarin clotting time (ECT)) have been observed [see Dosage and Administration (2.1) ].

The following serious adverse reactions are described in more detail elsewhere in the labeling: Thromboembolic Risk [see Warnings and Precautions (5.1) ] Hypersensitivity Reactions [see Warnings and Precautions (5.3) ] Risks of Serious Adverse Reactions in Patients with Hereditary Fructose Intolerance due to Sorbitol Excipient [see Warnings and Precautions (5.4) ] In healthy volunteers, the most frequently reported adverse reactions in ≥5% of subjects treated with idarucizumab was headache. ( 6.1 ) In patients, the most frequently reported adverse reactions in ≥5% of patients treated with idarucizumab were constipation and nausea. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Boehringer Ingelheim Pharmaceuticals, Inc. at 1-800-542-6257 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. In three healthy volunteer clinical trials, 224 subjects were treated with idarucizumab. In these trials, during the treatment period, the overall frequency of adverse events was similar between idarucizumab-treated subjects (55/224, 25%) and placebo-treated subjects (26/105, 25%). Among those subjects treated with idarucizumab, adverse reactions reported in ≥5% of subjects was headache (12/224, 5%).

8.1 Pregnancy Risk Summary There are no available data on PRAXBIND use in pregnant women to inform a drug-associated risk of major birth defects and miscarriage. Animal reproductive and development studies have not been conducted with idarucizumab. It is also not known whether PRAXBIND can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. PRAXBIND should be given to a pregnant woman only if clearly needed. The background risk of major birth defects and miscarriage for the indicated population is unknown. Adverse outcomes in pregnancy occur regardless of the health of the mother or the use of medications. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. 8.2 Lactation Risk Summary There are no data on the effects of PRAXBIND on the breastfed child or on milk production. It is not known whether idarucizumab is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when PRAXBIND is administered to a nursing woman. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for PRAXBIND and any potential adverse effects on the breastfed child from PRAXBIND or from the underlying maternal condition.

Metabolism

There were no obvious differences in the idarucizumab plasma concentration time profiles when idarucizumab was administered alone or after pretreatment with dabigatran. A dose-dependent increase in the fraction of unchanged idarucizumab excreted in urine was observed.

• Oct 16, 2015BLABLA761025Boehringer Ingelheim

1. 1Death16912%
2. 2Haemorrhage1198.3%
3. 3Gastrointestinal Haemorrhage815.7%
4. 4Cerebral Haemorrhage785.5%
5. 5Haemorrhage Intracranial674.7%
6. 6Drug Ineffective644.5%
7. 7Multiple Organ Dysfunction Syndrome624.3%
8. 8Acute Kidney Injury483.4%
9. 9Sepsis463.2%
10. 10Ischaemic Stroke453.2%
11. 11Pneumonia412.9%
12. 12Shock Haemorrhagic392.7%
13. 13Cerebrovascular Accident342.4%
14. 14Septic Shock332.3%
15. 15Cardiac Failure312.2%

The 10 most recently updated of 16 ClinicalTrials.gov registrations naming Idarucizumab as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• This Study Looks at the Effects of Idarucizumab in Patients Who Take Dabigatran and Need Emergency Surgery or Are Bleeding
  Completed · Phase 3 · Interventional · 19 enrolled · Boehringer Ingelheim
  NCT03343704updated 2025-02-25
• Registration of Idarucizumab for Patients with IntraCranial Hemorrhage
  Completed · Observational · 104 enrolled · University Hospital, Essen
  NCT04062097updated 2024-12-09
• PraxbindTM India PMS Program
  Completed · Observational · 5 enrolled · Boehringer Ingelheim
  NCT03359889updated 2023-08-25
• All-Case Surveillance of Prizbind®
  Completed · Observational · 1,402 enrolled · Boehringer Ingelheim
  NCT02946931updated 2022-09-09
• Japanese Pradaxa PMS, Long Term
  Completed · Observational · 5,660 enrolled · Boehringer Ingelheim
  NCT03175198updated 2022-04-06
• Observational Study to Evaluate Safety of Idarucizumab in Pediatric Patients
  Withdrawn · Observational · 0 enrolled · Boehringer Ingelheim
  NCT02798107updated 2021-11-18
• Reversal Agent Use in Patients Treated With Direct Oral Anticoagulants or Vitamin K Antagonists (RADOA). Focus on New Antidots
  Withdrawn · Observational · 0 enrolled · Cardioangiologisches Centrum Bethanien
  NCT03537521updated 2020-07-17
• Reversal Agent Use in Patients Treated With Direct Oral Anticoagulants or Vitamin K Antagonists
  Completed · Observational · 272 enrolled · Cardioangiologisches Centrum Bethanien
  NCT01722786updated 2020-07-16
• Reversal Dabigatran Anticoagulant Effect With Idarucizumab
  Completed · Phase 3 · Interventional · 1 enrolled · Boehringer Ingelheim
  NCT02815670updated 2020-04-14
• Study to Investigate the Pharmacokinetics (PK) and Pharmacodynamics (PD) of Idarucizumab in Chinese Healthy Male and Female Volunteers Who Had Taken Dabigatran Etexilate and Whose Plasma Concentrations of Dabigatran Were at or Close to Steady State
  Completed · Phase 1 · Interventional · 12 enrolled · Boehringer Ingelheim
  NCT03086356updated 2019-03-08

Frequently asked questions

How does Idarucizumab work?

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.

What is Idarucizumab used for?

According to FDA labeling, Idarucizumab carries indications including: PRAXBIND is indicated in patients treated with Pradaxa when reversal of the anticoagulant effects of dabigatran is needed: For emergency surgery/urgent procedures In life-threatening or uncontrolled bleeding PRAXBIND is a humanized monoclonal antibody fragment (Fab) indicated in patients treated with Pradaxa ® when reversal of the anticoagulant effects of dabigatran is needed: For emergency surgery/urgent procedures In life-threatening or uncontrolled bleeding ( 1 ). This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Idarucizumab?

Idarucizumab is classified as Antidotes, Humanized Monoclonal Antibody Fragment, Antibody Interactions.

What are the brand names for Idarucizumab?

Idarucizumab is marketed under brand names including Praxbind.

What are the contraindications for Idarucizumab?

Idarucizumab labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.