贝罗司他（Berotralstat）适应症及推荐剂量等介绍

FDA approval: Approved, first approved on December 3, 2020 Brand name:Orladeyo Generic name: berosalstat Dosage form: oral capsule (110 mg; 150 mg) Company: BioCryst Pharmaceuticals

Treatment: Hereditary Angioedema

Berostat

Berotralstat (BCX 7353) is an oral, highly selective plasma kallikrein inhibitor indicated for the prevention of angioedema episodes in patients with HAE, supported by once-daily dosing.

Indications

Berotralstat is indicated for the prevention of hereditary angioedema (Hae) in adults and children over 12 years of age.

Berotralstat is not indicated for the treatment of HAE that has already occurred and should only be used for prevention.

Before taking this medication, tell your doctor if you have ever experienced:

Liver disease; kidney disease (or if you are on dialysis); Heart rhythm problems. Pregnant or breastfeeding.

Berotralstat is not intended for use by anyone under the age of 12.

Berotralstat Recommended Dosage and Administration

1. Recommended dosage

The recommended dose of Berotralstat is a 150 mg capsule taken orally once daily with food.

2. Recommended dosage for patients with liver impairment

In patients with mild hepatic impairment (liver function class A), no dose adjustment of Berotralstat is recommended. For patients with moderate or severe hepatic impairment (liver function class B or C), the recommended oral dose of Berotralstat capsules is 110 mg once daily with food.

3. Recommended dosage for concurrent use with P-gp or BCRP inhibitors

In patients taking long-term P-Gp or BCRP inhibitors (such as cyclosporine), the recommended dose of oral Berotralstat capsules is 110 mg once daily.

4. Dose adjustment in patients with persistent gastrointestinal reactions

Gastrointestinal reactions may occur in patients receiving Berotralstat. If gastrointestinal events persist, consider taking a 110 mg capsule once daily with food.

5. How to take medicine Take Berotralstat exactly as your doctor tells you.

Take 1 capsule orally once daily with food.

Berotralstat side effects

Signs of an allergic reaction: Signs of an allergic reaction, such as rash; hives; itching; redness, swelling, or flaking of the skin with or without fever; wheezing; tightness in the chest or throat; difficulty breathing, swallowing, or speaking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Berotralstat Warnings and Precautions

1. Risk of QT prolongation at higher than recommended doses

Berotralstat should not be used to treat acute attacks of HAE. Additional once daily doses or doses higher than 150 mg of Berotralstat are not recommended. A concentration-dependent increase in QT was observed at doses above the recommended daily dose of 150 mg.

2. Drug interactions

Inform patients that Berotralstat may interact with other medications. Advise patients to report the use of any other prescription or over-the-counter medications or herbal products to their physician.

3. Not suitable for acute treatment of acute ischemic encephalopathy attack

Patients are advised to take commonly used rescue medications to treat acute ischemic encephalopathy attacks. Inform patients that the safety and effectiveness of using berotralstat as an acute treatment for HAE attacks has not been established. Advise patients not to take daily doses greater than 150 mg or additional doses of Berotralstat once daily to treat acute exacerbations of HAE due to the risk of QT prolongation.