Cytochrome P450 2D6 Inhibitors

Cytochrome P450 3A4 Inhibitors

Kallikrein Inhibitors

P-Glycoprotein Inhibitors

Plasma Kallikrein Inhibitor

<section class="Section" data-sectioncode="34089-3"><a name="S11"></a><a name="section-9"></a><p></p><h1>11 DESCRIPTION</h1><p class="First">ORLADEYO (berotralstat) capsules is a plasma kallikrein inhibitor. Berotralstat is presented as the dihydrochloride salt with the chemical name 1-[3-(aminomethyl)phenyl]-<span class="Italics">N</span>-(5-{(<span class="Italics">R</span>)-(3-cyanophenyl)[(cyclopropylmethyl)amino]methyl}-2-fluorophenyl)-3-(trifluoromethyl)-1<span class="Italics">H</span>-pyrazole-5-carboxamide dihydrochloride. The chemical structure is:</p><div class="Figure"><img alt="Chemical Structure" src="orladeyo-01.jpg"/></div><p>Berotralstat dihydrochloride is a white to off-white powder that is soluble in water at pH ≤4. The molecular formula is C<span class="Sub">30</span>H<span class="Sub">26</span>F<span class="Sub">4</span>N<span class="Sub">6</span>O ∙ 2HCl and the molecular weight is 635.49 (dihydrochloride).</p><p>ORLADEYO is supplied as 150 mg (equivalent to 169.4 mg berotralstat dihydrochloride) and 110 mg (equivalent to 124.3 mg berotralstat dihydrochloride) hard gelatin capsules for oral administration. Each capsule contains the active ingredient berotralstat dihydrochloride and the inactive ingredients colloidal silicon dioxide, crospovidone, magnesium stearate, and pregelatinized starch.</p></section>

Orladeyo

berotralstat

berotralstat 110 MG Oral Capsule

berotralstat 110 MG Oral Capsule [Orladeyo]

berotralstat 150 MG Oral Capsule

berotralstat 150 MG Oral Capsule [Orladeyo]

Bradykinin B2 Receptor Antagonist

Bradykinin B2 Receptor Antagonists

Hereditary Angioedemas

<section class="Section" data-sectioncode="34089-3"><a name="ID58"></a><a name="section-10"></a><p></p><h1>11 DESCRIPTION</h1><p class="First"><a name="ID59"></a>SAJAZIR (icatibant) is a synthetic decapeptide with five non-proteinogenic amino acids. The chemical structure of icatibant acetate is presented in Figure 1.</p><p><span class="Bold">Figure 1 Chemical Structure</span></p><div class="Figure"><img alt="Image" src="e8f64c57-bbfd-44de-8fd9-38d4c4d80638-01.jpg"/></div><p><a name="ID61"></a>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</p><p>SAJAZIR (icatibant) injection 30 mg/3ml (10 mg/mL) is provided as a sterile, isotonic, and buffered solution of icatibant acetate in a single-dose, prefilled syringe for subcutaneous administration. Each mL of the solution contains 10 mg of icatibant (free base) which is equivalent to 11.38 mg of icatibant acetate. Each prefilled syringe delivers 3 mL of solution equivalent to a 30 mg icatibant dose. The solution is clear and colorless. </p><p>The solution also contains sodium chloride (isotonicity reagent), glacial acetic acid (pH adjuster), sodium hydroxide (pH adjuster) and water for injection with a pH of approximately 5.5. The solution does not contain preservatives.</p><p> </p><p>Pharmacological class: Icatibant is a bradykinin B2 receptor antagonist.</p></section>

SAJAZIR

3 ML icatibant 10 MG/ML Prefilled Syringe

3 ML icatibant 10 MG/ML Prefilled Syringe [Firazyr]

3 ML icatibant 10 MG/ML Prefilled Syringe [Sajazir]

Firazyr

Sajazir

icatibant

Orladeyo is prescribed to prevent hereditary angioedema (HAE) attacks in individuals aged 12 and above.

It should not be used to treat an ongoing HAE attack.

The safety and effectiveness of Orladeyo in children under 12 years of age are currently unknown.

Report Adverse Event

Prescribing Information

Medication Guide

Medication Guide: Spanish

Submit MSL Request 

Pharmacy List 

Coverage Authorization Request 

Coverage Authorization Appeal 

Orladeyo Start Form 

Enroll in Patient Savings Program 

Bridge Program 

Other HCP Resources 

About Orladeyo

Side Effects

Comprehensive Support Program 

Patient Stories 

Instructions For Use: Hereditary Angioedema (HAE)

Patient Brochure

Doctor Discussion Guide: Patients Not Yet Taking Preventative Therapy

Doctor Discussion Guide: Currently Taking Preventative Therapy

Orladeyo Mentor Program Brochure

Patient Resources: Orladeyo Educational Classes

Orladeyo Follow Up Discussion Guide

SAJAZIR (icatibant) injection is a bradykinin B2 receptor antagonist indicated for
treatment of acute attacks of hereditary angioedema (HAE) in adults 18 years of
age and older.

Orladeyo®(berotralstat)	Sajazir®(icatibant)

Prescription Only Orladeyo is prescribed to prevent hereditary angioedema (HAE) attacks in individuals aged 12 and above. It should not be used to treat an ongoing HAE attack. The safety and...	Prescription Only SAJAZIR (icatibant) injection is a bradykinin B2 receptor antagonist indicated for treatment of acute attacks of hereditary angioedema (HAE) in adults 18 years of age and...
Dosage & Administration
Administration
Oral. Learn more.	Subcutaneous. Learn more.
Dosing
One capsule (150 mg) taken orally once daily with food.. Learn more.	30 mg injected subcutaneously in the abdominal area. If response is inadequate or symptoms recur, additional injections of 30 mg may be administered at intervals of at least 6 hours. . Learn more.
Latin Shorthand
1 capsule po qd w/food.. Learn more.	30 mg SC (subcutaneous) in abdomen. If inadequate response or recurring symptoms, administer additional 30 mg injections at ≥6-hour intervals.. Learn more.
Financial Assistance
Out-Of-Pocket Costs With Copay Card
$0. Learn more.	Learn more.
Annual Cap
Learn more.	Learn more.
Assistance Expiration
Calendar year. Learn more.	Learn more.
Generics
No lower-cost generic available	No lower-cost generic available
Physician Advisory
Adverse Reactions
Most common adverse reactions (≥10%) are abdominal pain, vomiting, diarrhea, back pain, and gastroesophageal reflux disease.. Learn more.	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. . Learn more.
Mechanism of Actions (MoA)
Drugs used in Hereditary Angioedema. Learn more.	Drugs used in Hereditary Angioedema. Learn more.
Special Populations

Orladeyo® Alternatives