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]

<section class="Section" data-sectioncode="34089-3"><a name="S11"></a><a name="section-10"></a><p></p><h1>11 DESCRIPTION</h1><p class="First">Lanadelumab-flyo, a plasma kallikrein inhibitor, is a non-plasma derived, recombinant, fully human, monoclonal antibody (IgG1/κ-light chain) produced in Chinese Hamster Ovary (CHO) cells. Based on the amino acid sequence, the molecular weight of the non-glycosylated lanadelumab-flyo is 146 kDa. The calculated molecular mass of the fully reduced light chain is 23 kDa. The calculated molecular mass of the fully reduced and non-glycosylated heavy chain is 49 kDa.</p><p>TAKHZYRO (lanadelumab-flyo) injection is a sterile, preservative-free, clear to slightly opalescent, colorless to slightly yellow solution for subcutaneous use.</p><p>Each mL of ready-to-use TAKHZYRO solution contains 150 mg of lanadelumab-flyo, citric acid monohydrate (4.1 mg), L-histidine (7.8 mg), polysorbate 80 (0.1 mg), sodium chloride (5.3 mg), sodium phosphate dibasic dihydrate (5.3 mg), and Water for Injection, USP. The solution has a pH of approximately 6.0.</p></section>

TAKHZYRO

1 ML lanadelumab-flyo 150 MG/ML Prefilled Syringe

1 ML lanadelumab-flyo 150 MG/ML Prefilled Syringe [Takhzyro]

2 ML lanadelumab-flyo 150 MG/ML Injection

2 ML lanadelumab-flyo 150 MG/ML Injection [Takhzyro]

2 ML lanadelumab-flyo 150 MG/ML Prefilled Syringe

2 ML lanadelumab-flyo 150 MG/ML Prefilled Syringe [Takhzyro]

Takhzyro

lanadelumab

lanadelumab-flyo

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.

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Prescribing Information

Medication Guide

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About Orladeyo

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Instructions For Use: Hereditary Angioedema (HAE)

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Takhzyro is a monoclonal antibody that controls an overactive enzyme in individuals with hereditary angioedema, a rare genetic immune system disorder. It is prescribed to prevent angioedema attacks in patients aged 2 and above.

Hereditary angioedema leads to elevated bradykinin levels. Takhzyro (lanadelumab-flyo) effectively reduces bradykinin levels, mitigating swelling and associated angioedema symptoms.

Takhzyro injections are FDA-approved for patients aged 2 and older to prevent hereditary angioedema attacks.

Orladeyo®(berotralstat)	Takhzyro®(lanadelumab-flyo)

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 Takhzyro is a monoclonal antibody that controls an overactive enzyme in individuals with hereditary angioedema, a rare genetic immune system disorder. It is prescribed to prevent...
Dosage & Administration
Administration
Oral. Learn more.	Subcutaneous. Learn more.
Dosing
One capsule (150 mg) taken orally once daily with food.. Learn more.	Adult and pediatric patients 12 years of age and older: administer 300 mg every 2 weeks. 6 to less than 12 years of age: administer 150 mg every 2 weeks. Pediatric patients 2 to less than 6 years of age: administer 150 mg every 4 weeks.. Learn more.
Latin Shorthand
1 capsule po qd w/food.. Learn more.	Adult and pediatric patients (≥12 years): 300 mg every 2 weeks. Patients aged 6 to <12 years: 150 mg every 2 weeks. Patients aged 2 to <6 years: 150 mg every 4 weeks.. Learn more.
Financial Assistance
Out-Of-Pocket Costs With Copay Card
$0. Learn more.	$0. 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 common adverse reactions (≥10%) are injection site reactions, upper respiratory infections, headache, rash, dizziness, diarrhea, and myalgia.. Learn more.
Mechanism of Actions (MoA)
Drugs used in Hereditary Angioedema. Learn more.	Drugs used in Hereditary Angioedema. Learn more.
Special Populations

Orladeyo® Alternatives