Icatibant Acetate

Generic Name: icatibant acetate

Over-the-Counter (OTC)

Brand Names:

Firazyr

11 DESCRIPTION FIRAZYR (icatibant) is a synthetic decapeptide with five non-proteinogenic amino acids. The chemical structure of icatibant acetate is presented in Figure 1. Figure 1 Chemical Structure Chemical name: D-Arginyl-L-arginyl-L-prolyl-L[(4R)-4-hydroxyprolyl]-glycyl-L[3-(2-thienyl)alanyl]-L-seryl-D-(1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl)-L[(3aS,7aS)-octahydroindol-2-ylcarbonyl]-L-arginine, acetate salt FIRAZYR is provided as a sterile, isotonic, and buffered solution of icatibant a...

Overview

11 DESCRIPTION FIRAZYR (icatibant) is a synthetic decapeptide with five non-proteinogenic amino acids. The chemical structure of icatibant acetate is presented in Figure 1. Figure 1 Chemical Structure Chemical name: D-Arginyl-L-arginyl-L-prolyl-L[(4R)-4-hydroxyprolyl]-glycyl-L[3-(2-thienyl)alanyl]-L-seryl-D-(1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl)-L[(3aS,7aS)-octahydroindol-2-ylcarbonyl]-L-arginine, acetate salt FIRAZYR is provided as a sterile, isotonic, and buffered solution of icatibant a...

Uses

1 INDICATIONS AND USAGE FIRAZYR ® (icatibant) is indicated for the treatment of acute attacks of hereditary angioedema (HAE) in adults 18 years of age and older. FIRAZYR is a bradykinin B2 receptor antagonist indicated for treatment of acute attacks of hereditary angioedema (HAE) in adults 18 years of age and older. ( 1 )

Dosage

2 DOSAGE AND ADMINISTRATION 30 mg injected subcutaneously in the abdominal area. ( 2.1 ) If response is inadequate or symptoms recur, additional injections of 30 mg may be administered at intervals of at least 6 hours. ( 2.1 ) Do not administer more than 3 injections in 24 hours. ( 2.1 ) Patients may self-administer upon recognition of an HAE attack. ( 2.2 ) 2.1 Recommended Dosing The recommended dose of FIRAZYR is 30 mg administered by subcutaneous (SC) injection in the abdominal area. Additional doses may be administered at intervals of at least 6 hours if response is inadequate or if symptoms recur. No more than 3 doses may be administered in any 24 hour period.

Side Effects

6 ADVERSE REACTIONS The most commonly reported adverse reactions were injection site reactions, which occurred in almost all patients (97%) in clinical trials. Other common adverse reactions occurring in greater than 1% of patients included pyrexia, transaminase increase, dizziness, and rash. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Takeda Pharmaceuticals America, Inc. at 1-877-TAKEDA-7 (1-877-825-3327) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience The safety of icatibant was evaluated in three controlled trials that included 223 patients who received FIRAZYR 30 mg (n=113), placebo (n=75), or comparator (n=38). The mean age at study entry was 38 years (range 18 to 83 years), 64% were female, and 95% were white.

Interactions

7 DRUG INTERACTIONS 7.1 ACE Inhibitors FIRAZYR is a bradykinin B2 receptor antagonist and thereby has the potential to have a pharmacodynamic interaction with ACE inhibitors where FIRAZYR may attenuate the antihypertensive effect of ACE inhibitors. Clinical trials to date have excluded subjects taking ACE inhibitors.

Warnings

5 WARNINGS AND PRECAUTIONS Laryngeal attacks: Following treatment of laryngeal attacks with FIRAZYR, advise patients to seek immediate medical attention. ( 5.1 ) 5.1 Laryngeal Attacks Given the potential for airway obstruction during acute laryngeal HAE attacks, patients should be advised to seek medical attention in an appropriate healthcare facility immediately in addition to treatment with FIRAZYR. 4 CONTRAINDICATIONS None. None ( 4 )

Pregnancy

8.1 Pregnancy Risk Summary Available data from published literature and the pharmacovigilance database with Firazyr (icatibant) use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. In animal reproduction studies, icatibant, administered by the subcutaneous route during the period of organogenesis, did not cause structural abnormalities in rats or rabbits; however, premature birth and abortion were observed in rabbits at doses approximately 0.025 times the maximum recommended human dose (MRHD) and higher.

Storage

16.2 Storage and Handling Keep out of the reach of children. Store between 2 - 25° C (36 - 77° F). Do not freeze. Store in carton until time of administration.

Frequently Asked Questions

What is Icatibant Acetate used for?

1 INDICATIONS AND USAGE FIRAZYR ® (icatibant) is indicated for the treatment of acute attacks of hereditary angioedema (HAE) in adults 18 years of age and older. FIRAZYR is a bradykinin B2 receptor antagonist indicated for treatment of acute attacks of hereditary angioedema (HAE) in adults 18 years of age and older. ( 1 )

What are the side effects of Icatibant Acetate?

6 ADVERSE REACTIONS The most commonly reported adverse reactions were injection site reactions, which occurred in almost all patients (97%) in clinical trials. Other common adverse reactions occurring in greater than 1% of patients included pyrexia, transaminase increase, dizziness, and rash. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Takeda Pharmaceuticals America, Inc. at 1-877-TAKEDA-7 (1-877-825-3327) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience The safety of icatibant was evaluated in three controlled trials that included 223 patients who received FIRAZYR 30 mg (n=113), placebo (n=75), or comparator (n=38). The mean age at study entry was 38 years (range 18 to 83 years), 64% were female, and 95% were white.

Can I take Icatibant Acetate during pregnancy?

8.1 Pregnancy Risk Summary Available data from published literature and the pharmacovigilance database with Firazyr (icatibant) use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. In animal reproduction studies, icatibant, administered by the subcutaneous route during the period of organogenesis, did not cause structural abnormalities in rats or rabbits; however, premature birth and abortion were observed in rabbits at doses approximately 0.025 times the maximum recommended human dose (MRHD) and higher.

What are the important warnings for Icatibant Acetate?

5 WARNINGS AND PRECAUTIONS Laryngeal attacks: Following treatment of laryngeal attacks with FIRAZYR, advise patients to seek immediate medical attention. ( 5.1 ) 5.1 Laryngeal Attacks Given the potential for airway obstruction during acute laryngeal HAE attacks, patients should be advised to seek medical attention in an appropriate healthcare facility immediately in addition to treatment with FIRAZYR. 4 CONTRAINDICATIONS None. None ( 4 )

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Medical Disclaimer

This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.